基本描述

产品名称	Recombinant Human Estrogen Receptor alpha Protein
别名	重组人Estrogen Receptor alpha蛋白 \| 重组人类雌激素受体α蛋白
英文别名	Estrogen Receptor alpha \| ER-alpha \| Estradiol receptor \| Nuclear receptor subfamily 3 group A member 1 \| ER \| Era \| ESR \| ESRA \| ESTRR \| NR3A \| 17/654 isoform \| 7/819 2 isoform \| 7/822 isoform \| 8/901 isoform \| 8*/941 isoform \| DKFZp686N23123 \| ER al
规格或纯度	Carrier Free, Azide Free, ≥90%(SDS-PAGE)
产品介绍	Purity:>90%, by SDS-PAGE visualized with Coomassie® Blue Staining. Description： ER alpha (Estrogen receptor alpha; also Estradiol receptor and NR3A1) is a 65-70 kDa member of the NR3 subfamily, nuclear hormone receptor family of proteins. It is widely expressed, and serves as a strong activator of estrogen-responsive genes. ER alpha is normally quiescent and bound to heat-shock proteins and immunophilins. Following beta -estradiol binding, it becomes activated, either homodimerizes or heterodimerizes with ER beta, and binds to DNA with multiple coactivators. Human ER alpha is 595 amino acids (aa) in length. It contains a DNA binding region (aa 185-250), three NLSs (aa 256-260; 266-271; 299-303), a steroid-binding site (aa 351-543), a dimerization motif (aa 497-518), and an O-GlcNAc attachment around Thr575. Major phosphorylation sites exist at Tyr537, Ser167 and Ser118. Multiple splice forms exist. There is an 80 kDa isoform that shows a substitution (duplication) of aa 412-517 for Asp411, a second isoform with a deletion of aa 255-366, a third isoform with a deletion of aa 152-412, and a fourth isoform that shows a Thr substitution for aa 152-595. Human ER alpha is only 46% aa identical to human ER beta. Over aa 1-116, human ER alpha shares 85% aa identity with mouse ER alpha.
内毒素水平	<1.0 EU/μg
表达系统	E. coli
种属	人(Human)
氨基酸	1-185 aa
序列	MHHHHHHMTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYC
蛋白标签	N-His
无载体	Yes
无动物源	No
Accession #	P03372
来源	重组表达
预测分子量	21.0 kDa
SDS-PAGE	24.8kDa and 47.1 kDa, reducing conditions; 24.8kDa and 47.1 kDa, non-reducing conditions

AI解读

图片

SDS-PAGE: Recombinant Human Estrogen Receptor alpha protein (rp175926)

Recombinant Human Estrogen Receptor alpha protein (rp175926) - SDS-PAGE
Recombinant Human Estrogen Receptor alpha protein was resolved with SDS-PAGE under reducing (R) and non-reducing (N) conditions and visualized by Coomassie® Blue staining, showing two bands at 24.8 and 47.1 kDa.

产品规格参数

物理形态	冻干(Lyophilized)
储存缓冲液	Lyophilized from 20mM Tris,400mM NaCl, 500mM Imidzole, 8M Urea, pH 8.0
复溶	We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Reconstitute at 0.5 mg/mL in sterile distilled water. Stock solutions should be apportioned into working aliquots and stored at ≤ -20 °C. Further dilutions should be made in appropriate buffered solutions.
储存温度	-20°C储存,避免反复冻融
运输条件	超低温冰袋运输
稳定性与储存	在 -20°C 下可保存 1 年。避免冷冻/解冻循环。
分子类型	蛋白质

技术规格说明书

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

输入批号以搜索分析图谱:

通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！

找到2个结果

批号(Lot Number)	证书类型	日期	货号
ZJ23F1101874	分析证书	23-12-13	rp175926
ZJ23F1101873	分析证书	23-12-13	rp175926

参考文献

1. Adamczyk M, Reddy RE, Yu Z.. (2002) Synthesis of a novel fluorescent probe for estrogen receptor.. Bioorg Med Chem Lett, 12 (9): (1283-1285). [PMID:11965371] [10.1016/s0960-894x(02)00144-0]
2. Kim YW, Mobley JA, Brueggemeier RW.. (2003) Synthesis and estrogen receptor binding affinities of 7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-ones containing a basic side chain.. Bioorg Med Chem Lett, 13 (8): (1475-1478). [PMID:12668015] [10.1016/s0960-894x(03)00132-x]
3. Lobaccaro C, Pons JF, Duchesne MJ, Auzou G, Pons M, Nique F, Teutsch G, Borgna JL.. (1997) Steroidal affinity labels of the estrogen receptor. 3. Estradiol 11 beta-n-alkyl derivatives bearing a terminal electrophilic group: antiestrogenic and cytotoxic properties.. J Med Chem, 40 (14): (2217-2227). [PMID:9216841] [10.1021/jm970019l]
4. Grese TA, Pennington LD, Sluka JP, Adrian MD, Cole HW, Fuson TR, Magee DE, Phillips DL, Rowley ER, Shetler PK, Short LL, Venugopalan M, Yang NN, Sato M, Glasebrook AL, Bryant HU.. (1998) Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators.. J Med Chem, 41 (8): (1272-1283). [PMID:9548817] [10.1021/jm970688z]
5. Fuhrmann U, Hess-Stumpp H, Cleve A, Neef G, Schwede W, Hoffmann J, Fritzemeier KH, Chwalisz K.. (2000) Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.. J Med Chem, 43 (26): (5010-5016). [PMID:11150172] [10.1021/jm001000c]
6. Schopfer U, Schoeffter P, Bischoff SF, Nozulak J, Feuerbach D, Floersheim P.. (2002) Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.. J Med Chem, 45 (7): (1399-1401). [PMID:11906280] [10.1021/jm015577l]
7. Bologa CG, Revankar CM, Young SM, Edwards BS, Arterburn JB, Kiselyov AS, Parker MA, Tkachenko SE, Savchuck NP, Sklar LA et al.. (2006) Virtual and biomolecular screening converge on a selective agonist for GPR30.. Nat Chem Biol, 2 (4): (207-12). [PMID:16520733] [10.1021/op500134e]
8. Dennis MK, Burai R, Ramesh C, Petrie WK, Alcon SN, Nayak TK, Bologa CG, Leitao A, Brailoiu E, Deliu E et al.. (2009) In vivo effects of a GPR30 antagonist.. Nat Chem Biol, 5 (6): (421-7). [PMID:19430488] [10.1021/op500134e]
9. Qi C, Chang J, Zhu Y, Yeldandi AV, Rao SM, Zhu YJ. (2002) Identification of protein arginine methyltransferase 2 as a coactivator for estrogen receptor alpha.. J Biol Chem, 277 (32): (28624-30). [PMID:12039952] [10.1021/op500134e]
10. Shao W, Halachmi S, Brown M. (2002) ERAP140, a conserved tissue-specific nuclear receptor coactivator.. Mol Cell Biol, 22 (10): (3358-72). [PMID:11971969] [10.1021/op500134e]
11. Sauvé F, McBroom LD, Gallant J, Moraitis AN, Labrie F, Giguère V. (2001) CIA, a novel estrogen receptor coactivator with a bifunctional nuclear receptor interacting determinant.. Mol Cell Biol, 21 (1): (343-53). [PMID:11113208] [10.1021/op500134e]
12. Sun J, Meyers MJ, Fink BE, Rajendran R, Katzenellenbogen JA, Katzenellenbogen BS. (1999) Novel ligands that function as selective estrogens or antiestrogens for estrogen receptor-alpha or estrogen receptor-beta.. Endocrinology, 140 (2): (800-4). [PMID:9927308] [10.1021/op500134e]
13. Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL. (1998) The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen.. Cell, 95 (7): (927-37). [PMID:9875847] [10.1021/op500134e]
14. Greene GL, Gilna P, Waterfield M, Baker A, Hort Y, Shine J. (1986) Sequence and expression of human estrogen receptor complementary DNA.. Science, 231 (4742): (1150-4). [PMID:3753802] [10.1021/op500134e]
15. Teyssier C, Belguise K, Galtier F, Chalbos D. (2001) Characterization of the physical interaction between estrogen receptor alpha and JUN proteins.. J Biol Chem, 276 (39): (36361-9). [PMID:11477071] [10.1021/op500134e]
16. Flouriot G, Brand H, Denger S, Metivier R, Kos M, Reid G, Sonntag-Buck V, Gannon F. (2000) Identification of a new isoform of the human estrogen receptor-alpha (hER-alpha) that is encoded by distinct transcripts and that is able to repress hER-alpha activation function 1.. EMBO J, 19 (17): (4688-700). [PMID:10970861] [10.1021/op500134e]
17. Hu YC, Shyr CR, Che W, Mu XM, Kim E, Chang C. (2002) Suppression of estrogen receptor-mediated transcription and cell growth by interaction with TR2 orphan receptor.. J Biol Chem, 277 (37): (33571-9). [PMID:12093804] [10.1021/op500134e]
18. Compton DR, Sheng S, Carlson KE, Rebacz NA, Lee IY, Katzenellenbogen BS, Katzenellenbogen JA. (2004) Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity.. J Med Chem, 47 (24): (5872-93). [PMID:15537344] [10.1021/op500134e]
19. Malamas MS, Manas ES, McDevitt RE, Gunawan I, Xu ZB, Collini MD, Miller CP, Dinh T, Henderson RA, Keith JC et al.. (2004) Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.. J Med Chem, 47 (21): (5021-40). [PMID:15456246] [10.1021/op500134e]
20. Kinoyama I, Taniguchi N, Toyoshima A, Nozawa E, Kamikubo T, Imamura M, Matsuhisa A, Samizu K, Kawanimani E, Niimi T et al.. (2006) (+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.. J Med Chem, 49 (2): (716-26). [PMID:16420057] [10.1021/op500134e]
21. Le Romancer M, Treilleux I, Leconte N, Robin-Lespinasse Y, Sentis S, Bouchekioua-Bouzaghou K, Goddard S, Gobert-Gosse S, Corbo L. (2008) Regulation of estrogen rapid signaling through arginine methylation by PRMT1.. Mol Cell, 31 (2): (212-21). [PMID:18657504] [10.1021/op500134e]
22. Millan DS, Ballard SA, Chunn S, Dybowski JA, Fulton CK, Glossop PA, Guillabert E, Hewson CA, Jones RM, Lamb DJ et al.. (2011) Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.. Bioorg Med Chem Lett, 21 (19): (5826-30). [PMID:21880489] [10.1021/op500134e]
23. Renaud J, Bischoff SF, Buhl T, Floersheim P, Fournier B, Geiser M, Halleux C, Kallen J, Keller H, Ramage P. (2005) Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.. J Med Chem, 48 (2): (364-79). [PMID:15658851] [10.1021/op500134e]
24. Fensome A, Adams WR, Adams AL, Berrodin TJ, Cohen J, Huselton C, Illenberger A, Kern JC, Hudak VA, Marella MA et al.. (2008) Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).. J Med Chem, 51 (6): (1861-73). [PMID:18318463] [10.1021/op500134e]
25. Maruyama K, Nakamura M, Tomoshige S, Sugita K, Makishima M, Hashimoto Y, Ishikawa M. (2013) Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERα-selective antagonist.. Bioorg Med Chem Lett, 23 (14): (4031-6). [PMID:23768907] [10.1021/op500134e]
26. Coombs TC, Tanega C, Shen M, Wang JL, Auld DS, Gerritz SW, Schoenen FJ, Thomas CJ, Aubé J. (2013) Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.. Bioorg Med Chem Lett, 23 (12): (3654-61). [PMID:23642479] [10.1021/op500134e]
27. Hsiao PW, Fryer CJ, Trotter KW, Wang W, Archer TK. (2003) BAF60a mediates critical interactions between nuclear receptors and the BRG1 chromatin-remodeling complex for transactivation.. Mol Cell Biol, 23 (17): (6210-20). [PMID:12917342] [10.1021/op500134e]
28. Chan SW, Hong W. (2001) Retinoblastoma-binding protein 2 (Rbp2) potentiates nuclear hormone receptor-mediated transcription.. J Biol Chem, 276 (30): (28402-12). [PMID:11358960] [10.1021/op500134e]
29. Quaynor SD, Stradtman Jr EW, Kim HG, Shen Y, Chorich LP, Schreihofer DA, Layman LC. (2013) Delayed puberty and estrogen resistance in a woman with estrogen receptor α variant.. N Engl J Med, 369 (2): (164-71). [PMID:23841731] [10.1021/op500134e]
30. McFarland K, Price DL, Davis CN, Ma JN, Bonhaus DW, Burstein ES, Olsson R. (2013) AC-186, a selective nonsteroidal estrogen receptor β agonist, shows gender specific neuroprotection in a Parkinson's disease rat model.. ACS Chem Neurosci, 4 (9): (1249-55). [PMID:23898966] [10.1021/op500134e]
31. Waters EM, Mitterling K, Spencer JL, Mazid S, McEwen BS, Milner TA. (2009) Estrogen receptor alpha and beta specific agonists regulate expression of synaptic proteins in rat hippocampus.. Brain Res, 1290 (13): (1-11). [PMID:19596275] [10.1021/op500134e]
32. Cvoro A, Tatomer D, Tee MK, Zogovic T, Harris HA, Leitman DC. (2008) Selective estrogen receptor-beta agonists repress transcription of proinflammatory genes.. J Immunol, 180 (1): (630-6). [PMID:18097065] [10.1021/op500134e]
33. Solt LA, Wang Y, Banerjee S, Hughes T, Kojetin DJ, Lundasen T, Shin Y, Liu J, Cameron MD, Noel R et al.. (2012) Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.. Nature, 485 (7396): (62-8). [PMID:22460951] [10.1021/op500134e]
34. Migliore M, Habrant D, Sasso O, Albani C, Bertozzi SM, Armirotti A, Piomelli D, Scarpelli R. (2016) Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies.. Eur J Med Chem, 109 (13): (216-37). [PMID:26774927] [10.1021/op500134e]
35. Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, Seitz P, Plouffe DM, Dharia NV, Tan J et al.. (2010) Spiroindolones, a potent compound class for the treatment of malaria.. Science, 329 (5996): (1175-80). [PMID:20813948] [10.1021/op500134e]
36. Lv W, Liu J, Lu D, Flockhart DA, Cushman M. (2013) Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.. J Med Chem, 56 (11): (4611-8). [PMID:23731360] [10.1021/op500134e]
37. Abdelsamie AS, Salah M, Siebenbürger L, Merabet A, Scheuer C, Frotscher M, Müller ST, Zierau O, Vollmer G, Menger MD et al.. (2019) Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis.. J Med Chem, 62 (15): (7289-7301). [PMID:31343176] [10.1021/op500134e]
38. Zou JX, Revenko AS, Li LB, Gemo AT, Chen HW. (2007) ANCCA, an estrogen-regulated AAA+ ATPase coactivator for ERalpha, is required for coregulator occupancy and chromatin modification.. Proc Natl Acad Sci USA, 104 (46): (18067-72). [PMID:17998543] [10.1021/op500134e]
39. Hu J, Hu B, Wang M, Xu F, Miao B, Yang CY, Wang M, Liu Z, Hayes DF, Chinnaswamy K et al.. (2019) Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER).. J Med Chem, 62 (3): (1420-1442). [PMID:30990042] [10.1021/op500134e]
40. El-Ahmad Y, Tabart M, Halley F, Certal V, Thompson F, Filoche-Rommé B, Gruss-Leleu F, Muller C, Brollo M, Fabien L et al.. (2020) Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer.. J Med Chem, 63 (2): (512-528). [PMID:31721572] [10.1021/acs.jmedchem.9b01293]
41. Chianelli D, Rucker PV, Roland J, Tully DC, Nelson J, Liu X, Bursulaya B, Hernandez ED, Wu J, Prashad M et al.. (2020) Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.. J Med Chem, 63 (8): (3868-3880). [PMID:31940200] [10.1021/op500134e]
42. Tria GS, Abrams T, Baird J, Burks HE, Firestone B, Gaither LA, Hamann LG, He G, Kirby CA, Kim S et al.. (2018) Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.. J Med Chem, 61 (7): (2837-2864). [PMID:29562737] [10.1021/op500134e]
43. Jeongsoo Yoo, Carmen S Dence, Terry L Sharp, John A Katzenellenbogen, Michael J Welch,. (2005-09-30) Synthesis of an estrogen receptor beta-selective radioligand: 5-[18F]fluoro-(2R,3S)-2,3-bis(4-hydroxyphenyl)pentanenitrile and comparison of in vivo distribution with 16alpha-[18F]fluoro-17beta-estradiol.. Journal of medicinal chemistry, 48 ((20)): ( 6366-6378 ). [PMID:16190762]
44. Koichiro Harada,Hideki Kubo,Yoshitaka Tomigahara,Kazuhiko Nishioka,Junya Takahashi,Mio Momose,Shinichi Inoue,Atsuyuki Kojima. (2009-12-04) Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.. Bioorganic & medicinal chemistry letters, 20 ((1)): (272-275). [PMID:19954971]
45. Stefan Starcević,Petra Brozic,Samo Turk,Jozko Cesar,Tea Lanisnik Rizner,Stanislav Gobec. (2010-12-09) Synthesis and biological evaluation of (6- and 7-phenyl) coumarin derivatives as selective nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1.. Journal of medicinal chemistry, 54 ((1)): (248-261). [PMID:21138273]
46. Simone Bertini,Andrea De Cupertinis,Carlotta Granchi,Barbara Bargagli,Tiziano Tuccinardi,Adriano Martinelli,Marco Macchia,Jillian R Gunther,Kathryn E Carlson,John A Katzenellenbogen,Filippo Minutolo. (2011-04-13) Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes.. European journal of medicinal chemistry, 46 ((6)): (2453-2462). [PMID:21481497]
47. H Matsuda,H Shimoda,T Morikawa,M Yoshikawa. (2001-07-19) Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity.. Bioorganic & medicinal chemistry letters, 11 ((14)): (1839-1842). [PMID:11459643]
48. Pascal Pigeon,Siden Top,Anne Vessières,Michel Huché,Elizabeth A Hillard,Emmanuel Salomon,Gérard Jaouen. (2005-04-15) Selective estrogen receptor modulators in the ruthenocene series. Synthesis and biological behavior.. Journal of medicinal chemistry, 48 ((8)): (2814-2821). [PMID:15828819]
49. Michael Waibel,Meri De Angelis,Fabio Stossi,Karen J Kieser,Kathryn E Carlson,Benita S Katzenellenbogen,John A Katzenellenbogen. (2009-03-17) Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta.. European journal of medicinal chemistry, 44 ((9)): (3412-3424). [PMID:19286283]
50. Satu Massinen,Kristiina Tammimies,Isabel Tapia-Páez,Hans Matsson,Marie-Estelle Hokkanen,Ola Söderberg,Ulf Landegren,Eero Castrén,Jan-Ake Gustafsson,Eckardt Treuter,Juha Kere. (2009-05-09) Functional interaction of DYX1C1 with estrogen receptors suggests involvement of hormonal pathways in dyslexia.. Human molecular genetics, 18 ((15)): (2802-2812). [PMID:19423554]
51. Alexander Oster,Tobias Klein,Ruth Werth,Patricia Kruchten,Emmanuel Bey,Matthias Negri,Sandrine Marchais-Oberwinkler,Martin Frotscher,Rolf W Hartmann. (2010-04-24) Novel estrone mimetics with high 17beta-HSD1 inhibitory activity.. Bioorganic & medicinal chemistry, 18 ((10)): (3494-3505). [PMID:20413314]
52. Xiaohui Liu,Keitaro Suyama,Junichi Shiki,Kohei Torikai,Takeru Nose,Miki Shimohigashi,Yasuyuki Shimohigashi. (2019-12-28) Bisphenol AF: Halogen bonding effect is a major driving force for the dual ERα-agonist and ERβ-antagonist activities.. Bioorganic & medicinal chemistry, 28 ((3)): (115274-115274). [PMID:31879182]
53. Tan Q, Birzin ET, Chan W, Tien Yang Y, Pai LY, Hayes EC, DaSilva CA, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.. (2004) Estrogen receptor ligands. Part 5: The SAR of dihydrobenzoxathiins containing modified basic side chains.. Bioorg Med Chem Lett, 14 (14): (3747-3751). [PMID:15203155] [10.1016/j.bmcl.2004.04.100]
54. Gagnon V, St-Germain ME, Descôteaux C, Provencher-Mandeville J, Parent S, Mandal SK, Asselin E, Bérubé G.. (2004) Biological evaluation of novel estrogen-platinum(II) hybrid molecules on uterine and ovarian cancers-molecular modeling studies.. Bioorg Med Chem Lett, 14 (23): (5919-5924). [PMID:15501069] [10.1016/j.bmcl.2004.09.015]
55. Zhao L, Brinton RD.. (2005) Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases.. J Med Chem, 48 (10): (3463-3466). [PMID:15887952] [10.1021/jm0490538]
56. Clegg NJ, Paruthiyil S, Leitman DC, Scanlan TS.. (2005) Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands.. J Med Chem, 48 (19): (5989-6003). [PMID:16162002] [10.1021/jm050226i]
57. Hummel CW, Geiser AG, Bryant HU, Cohen IR, Dally RD, Fong KC, Frank SA, Hinklin R, Jones SA, Lewis G, McCann DJ, Rudmann DG, Shepherd TA, Tian H, Wallace OB, Wang M, Wang Y, Dodge JA.. (2005) A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.. J Med Chem, 48 (22): (6772-6775). [PMID:16250633] [10.1021/jm050723z]
58. Wallace OB, Lauwers KS, Dodge JA, May SA, Calvin JR, Hinklin R, Bryant HU, Shetler PK, Adrian MD, Geiser AG, Sato M, Burris TP.. (2006) A selective estrogen receptor modulator for the treatment of hot flushes.. J Med Chem, 49 (3): (843-846). [PMID:16451049] [10.1021/jm0509795]
59. Tuccinardi T, Bertini S, Martinelli A, Minutolo F, Ortore G, Placanica G, Prota G, Rapposelli S, Carlson KE, Katzenellenbogen JA, Macchia M.. (2006) Synthesis of anthranylaldoxime derivatives as estrogen receptor ligands and computational prediction of binding modes.. J Med Chem, 49 (16): (5001-5012). [PMID:16884312] [10.1021/jm060560u]
60. Zhou HB, Comninos JS, Stossi F, Katzenellenbogen BS, Katzenellenbogen JA.. (2005) Synthesis and evaluation of estrogen receptor ligands with bridged oxabicyclic cores containing a diarylethylene motif: estrogen antagonists of unusual structure.. J Med Chem, 48 (23): (7261-7274). [PMID:16279785] [10.1021/jm0506773]
61. Richardson TI, Frank SA, Wang M, Clarke CA, Jones SA, Ying BP, Kohlman DT, Wallace OB, Shepherd TA, Dally RD, Palkowitz AD, Geiser AG, Bryant HU, Henck JW, Cohen IR, Rudmann DG, McCann DJ, Coutant DE, Oldham SW, Hummel CW, Fong KC, Hinklin R, Lewis G, Tian H, Dodge JA.. (2007) Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.. Bioorg Med Chem Lett, 17 (13): (3544-3549). [PMID:17482463] [10.1016/j.bmcl.2007.04.044]
62. Zhao L, Jin C, Mao Z, Gopinathan MB, Rehder K, Brinton RD.. (2007) Design, synthesis, and estrogenic activity of a novel estrogen receptor modulator--a hybrid structure of 17beta-estradiol and vitamin E in hippocampal neurons.. J Med Chem, 50 (18): (4471-4481). [PMID:17696335] [10.1021/jm070546x]
63. Dykstra KD, Guo L, Birzin ET, Chan W, Yang YT, Hayes EC, DaSilva CA, Pai LY, Mosley RT, Kraker B, Fitzgerald PM, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.. (2007) Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.. Bioorg Med Chem Lett, 17 (8): (2322-2328). [PMID:17289385] [10.1016/j.bmcl.2007.01.054]
64. Lin HR, Safo MK, Abraham DJ.. (2007) Identification of a series of tetrahydroisoquinoline derivatives as potential therapeutic agents for breast cancer.. Bioorg Med Chem Lett, 17 (9): (2581-2589). [PMID:17337183] [10.1016/j.bmcl.2007.02.002]
65. Frotscher M, Ziegler E, Marchais-Oberwinkler S, Kruchten P, Neugebauer A, Fetzer L, Scherer C, Müller-Vieira U, Messinger J, Thole H, Hartmann RW.. (2008) Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.. J Med Chem, 51 (7): (2158-2169). [PMID:18324762] [10.1021/jm701447v]
66. Bey E, Marchais-Oberwinkler S, Kruchten P, Frotscher M, Werth R, Oster A, Algül O, Neugebauer A, Hartmann RW.. (2008) Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.. Bioorg Med Chem, 16 (12): (6423-6435). [PMID:18514529] [10.1016/j.bmc.2008.04.073]
67. Akwabi-Ameyaw A, Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Jones SA, Kaldor I, Liu Y, Madauss KP, Marr HB, McFadyen RB, Miller AB, Navas F, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB.. (2008) Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.. Bioorg Med Chem Lett, 18 (15): (4339-4343). [PMID:18621523] [10.1016/j.bmcl.2008.06.073]
68. Marchais-Oberwinkler S, Kruchten P, Frotscher M, Ziegler E, Neugebauer A, Bhoga U, Bey E, Müller-Vieira U, Messinger J, Thole H, Hartmann RW.. (2008) Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics.. J Med Chem, 51 (15): (4685-4698). [PMID:18630892] [10.1021/jm800367k]
69. Bey E, Marchais-Oberwinkler S, Werth R, Negri M, Al-Soud YA, Kruchten P, Oster A, Frotscher M, Birk B, Hartmann RW.. (2008) Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1).. J Med Chem, 51 (21): (6725-6739). [PMID:18855374] [10.1021/jm8006917]
70. LaFrate AL, Gunther JR, Carlson KE, Katzenellenbogen JA.. (2008) Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor.. Bioorg Med Chem, 16 (23): (10075-10084). [PMID:18976929] [10.1016/j.bmc.2008.10.007]
71. Zhou HB, Carlson KE, Stossi F, Katzenellenbogen BS, Katzenellenbogen JA.. (2009) Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity.. Bioorg Med Chem Lett, 19 (1): (108-110). [PMID:19014882] [10.1016/j.bmcl.2008.11.006]
72. Parent AA, Gunther JR, Katzenellenbogen JA.. (2008) Blocking estrogen signaling after the hormone: pyrimidine-core inhibitors of estrogen receptor-coactivator binding.. J Med Chem, 51 (20): (6512-6530). [PMID:18785725] [10.1021/jm800698b]
73. Flatt B, Martin R, Wang TL, Mahaney P, Murphy B, Gu XH, Foster P, Li J, Pircher P, Petrowski M, Schulman I, Westin S, Wrobel J, Yan G, Bischoff E, Daige C, Mohan R.. (2009) Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR).. J Med Chem, 52 (4): (904-907). [PMID:19159286] [10.1021/jm8014124]
74. Barrett I, Meegan MJ, Hughes RB, Carr M, Knox AJ, Artemenko N, Golfis G, Zisterer DM, Lloyd DG.. (2008) Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators.. Bioorg Med Chem, 16 (21): (9554-9573). [PMID:18835176] [10.1016/j.bmc.2008.09.035]
75. Asim M, El-Salfiti M, Qian Y, Choueiri C, Salari S, Cheng J, Shadnia H, Bal M, Christine Pratt MA, Carlson KE, Katzenellenbogen JA, Wright JS, Durst T.. (2009) Deconstructing estradiol: removal of B-ring generates compounds which are potent and subtype-selective estrogen receptor agonists.. Bioorg Med Chem Lett, 19 (4): (1250-1253). [PMID:19167882] [10.1016/j.bmcl.2008.12.080]
76. Trogden BG, Kim SH, Lee S, Katzenellenbogen JA.. (2009) Tethered indoles as functionalizable ligands for the estrogen receptor.. Bioorg Med Chem Lett, 19 (2): (485-488). [PMID:19059778] [10.1016/j.bmcl.2008.11.043]
77. Sarachine MJ, Janjic JM, Wipf P, Day BW.. (2009) Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor beta.. Bioorg Med Chem Lett, 19 (9): (2404-2408). [PMID:19356928] [10.1016/j.bmcl.2009.03.075]
78. Moon BS, Carlson KE, Katzenellenbogen JA, Choi TH, Chi DY, Kim JY, Cheon GJ, Koh HY, Lee KC, An G.. (2009) Synthesis and evaluation of aryl-substituted diarylpropionitriles, selective ligands for estrogen receptor beta, as positron-emission tomographic imaging agents.. Bioorg Med Chem, 17 (9): (3479-3488). [PMID:19359182] [10.1016/j.bmc.2009.02.064]
79. Liu W, Liu K, Wood HB, McCann ME, Doebber TW, Chang CH, Akiyama TE, Einstein M, Berger JP, Meinke PT.. (2009) Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.. J Med Chem, 52 (14): (4443-4453). [PMID:19530681] [10.1021/jm900367w]
80. LaFrate AL, Carlson KE, Katzenellenbogen JA.. (2009) Steroidal bivalent ligands for the estrogen receptor: design, synthesis, characterization and binding affinities.. Bioorg Med Chem, 17 (10): (3528-3535). [PMID:19394231] [10.1016/j.bmc.2009.04.016]
81. Lilienkampf A, Karkola S, Alho-Richmond S, Koskimies P, Johansson N, Huhtinen K, Vihko K, Wähälä K.. (2009) Synthesis and biological evaluation of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors based on a thieno[2,3-d]pyrimidin-4(3H)-one core.. J Med Chem, 52 (21): (6660-6671). [PMID:19824648] [10.1021/jm900928k]
82. Bey E, Marchais-Oberwinkler S, Negri M, Kruchten P, Oster A, Klein T, Spadaro A, Werth R, Frotscher M, Birk B, Hartmann RW.. (2009) New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: influence of additional substituents on 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitory activity and selectivity.. J Med Chem, 52 (21): (6724-6743). [PMID:19831396] [10.1021/jm901195w]
83. Ramesh C, Nayak TK, Burai R, Dennis MK, Hathaway HJ, Sklar LA, Prossnitz ER, Arterburn JB.. (2010) Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.. J Med Chem, 53 (3): (1004-1014). [PMID:20041667] [10.1021/jm9011802]
84. Möller G, Deluca D, Gege C, Rosinus A, Kowalik D, Peters O, Droescher P, Elger W, Adamski J, Hillisch A.. (2009) Structure-based design, synthesis and in vitro characterization of potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone.. Bioorg Med Chem Lett, 19 (23): (6740-6744). [PMID:19836949] [10.1016/j.bmcl.2009.09.113]
85. Mita Y, Dodo K, Noguchi-Yachide T, Miyachi H, Makishima M, Hashimoto Y, Ishikawa M.. (2010) LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.. Bioorg Med Chem Lett, 20 (5): (1712-1717). [PMID:20144545] [10.1016/j.bmcl.2010.01.079]
86. Maximov PY, Myers CB, Curpan RF, Lewis-Wambi JS, Jordan VC.. (2010) Structure-function relationships of estrogenic triphenylethylenes related to endoxifen and 4-hydroxytamoxifen.. J Med Chem, 53 (8): (3273-3283). [PMID:20334368] [10.1021/jm901907u]
87. Kieser KJ, Kim DW, Carlson KE, Katzenellenbogen BS, Katzenellenbogen JA.. (2010) Characterization of the pharmacophore properties of novel selective estrogen receptor downregulators (SERDs).. J Med Chem, 53 (8): (3320-3329). [PMID:20334372] [10.1021/jm100047k]
88. Rivera-Guevara C, Pérez-Alvarez V, García-Becerra R, Ordaz-Rosado D, Morales-Ríos MS, Hernández-Gallegos E, Cooney AJ, Bravo-Gómez ME, Larrea F, Camacho J.. (2010) Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.. Bioorg Med Chem, 18 (15): (5593-5601). [PMID:20621492] [10.1016/j.bmc.2010.06.039]
89. Jiang Q, Payton-Stewart F, Elliott S, Driver J, Rhodes LV, Zhang Q, Zheng S, Bhatnagar D, Boue SM, Collins-Burow BM, Sridhar J, Stevens C, McLachlan JA, Wiese TE, Burow ME, Wang G.. (2010) Effects of 7-O substitutions on estrogenic and anti-estrogenic activities of daidzein analogues in MCF-7 breast cancer cells.. J Med Chem, 53 (16): (6153-6163). [PMID:20669983] [10.1021/jm100610w]
90. Meyers MJ, Arhancet GB, Hockerman SL, Chen X, Long SA, Mahoney MW, Rico JR, Garland DJ, Blinn JR, Collins JT, Yang S, Huang HC, McGee KF, Wendling JM, Dietz JD, Payne MA, Homer BL, Heron MI, Reitz DB, Hu X.. (2010) Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.. J Med Chem, 53 (16): (5979-6002). [PMID:20672822] [10.1021/jm100505n]
91. Jain D, Koh JT.. (2010) A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements.. Bioorg Med Chem Lett, 20 (17): (5258-5261). [PMID:20659801] [10.1016/j.bmcl.2010.06.151]
92. Oster A, Hinsberger S, Werth R, Marchais-Oberwinkler S, Frotscher M, Hartmann RW.. (2010) Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases.. J Med Chem, 53 (22): (8176-8186). [PMID:20977238] [10.1021/jm101073q]
93. Wetzel M, Marchais-Oberwinkler S, Hartmann RW.. (2011) 17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold.. Bioorg Med Chem, 19 (2): (807-815). [PMID:21211981] [10.1016/j.bmc.2010.12.013]
94. Marchais-Oberwinkler S, Wetzel M, Ziegler E, Kruchten P, Werth R, Henn C, Hartmann RW, Frotscher M.. (2011) New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.. J Med Chem, 54 (2): (534-547). [PMID:21189020] [10.1021/jm1009082]
95. Wright JS, Shadnia H, Anderson JM, Durst T, Asim M, El-Salfiti M, Choueiri C, Pratt MA, Ruddy SC, Lau R, Carlson KE, Katzenellenbogen JA, O'Brien PJ, Wan L.. (2011) A-CD estrogens. I. Substituent effects, hormone potency, and receptor subtype selectivity in a new family of flexible estrogenic compounds.. J Med Chem, 54 (2): (433-448). [PMID:21190382] [10.1021/jm100513m]
96. Patch RJ, Searle LL, Kim AJ, De D, Zhu X, Askari HB, O'Neill JC, Abad MC, Rentzeperis D, Liu J, Kemmerer M, Lin L, Kasturi J, Geisler JG, Lenhard JM, Player MR, Gaul MD.. (2011) Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.. J Med Chem, 54 (3): (788-808). [PMID:21218783] [10.1021/jm101063h]
97. Xia G, Benmohamed R, Kim J, Arvanites AC, Morimoto RI, Ferrante RJ, Kirsch DR, Silverman RB.. (2011) Pyrimidine-2,4,6-trione derivatives and their inhibition of mutant SOD1-dependent protein aggregation. Toward a treatment for amyotrophic lateral sclerosis.. J Med Chem, 54 (7): (2409-2421). [PMID:21375347] [10.1021/jm101549k]
98. Katzenellenbogen JA.. (2011) The 2010 Philip S. Portoghese Medicinal Chemistry Lectureship: addressing the "core issue" in the design of estrogen receptor ligands.. J Med Chem, 54 (15): (5271-5282). [PMID:21707083] [10.1021/jm200801h]
99. Wetzel M, Marchais-Oberwinkler S, Perspicace E, Möller G, Adamski J, Hartmann RW.. (2011) Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors.. J Med Chem, 54 (21): (7547-7557). [PMID:21972996] [10.1021/jm2008453]
100. Xu K, Al-Soud YA, Wetzel M, Hartmann RW, Marchais-Oberwinkler S.. (2011) Triazole ring-opening leads to the discovery of potent nonsteroidal 17β-hydroxysteroid dehydrogenase type 2 inhibitors.. Eur J Med Chem, 46 (12): (5978-5990). [PMID:22037253] [10.1016/j.ejmech.2011.10.010]
101. Wetzel M, Gargano EM, Hinsberger S, Marchais-Oberwinkler S, Hartmann RW.. (2012) Discovery of a new class of bicyclic substituted hydroxyphenylmethanones as 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors for the treatment of osteoporosis.. Eur J Med Chem, 47 (1-17). [PMID:21945251] [10.1016/j.ejmech.2011.09.004]
102. Harada K, Kubo H, Tanaka A, Nishioka K.. (2012) Identification of oxazolidinediones and thiazolidinediones as potent 17β-hydroxysteroid dehydrogenase type 3 inhibitors.. Bioorg Med Chem Lett, 22 (1): (504-507). [PMID:22137341] [10.1016/j.bmcl.2011.10.095]
103. Olmsted SL, Tongcharoensirikul P, McCaskill E, Gandiaga K, Labaree D, Hochberg RB, Hanson RN.. (2012) Synthesis and evaluation of 17α-E-20-(heteroaryl)norpregn-1,3,5(10),20 tetraene-3,17β-diols [17α-(heteroaryl)vinyl estradiols] as ligands for the estrogen receptor-α ligand binding domain (ERα-LBD).. Bioorg Med Chem Lett, 22 (2): (977-979). [PMID:22178552] [10.1016/j.bmcl.2011.12.003]
104. Carroll VM, Jeyakumar M, Carlson KE, Katzenellenbogen JA.. (2012) Diarylpropionitrile (DPN) enantiomers: synthesis and evaluation of estrogen receptor β-selective ligands.. J Med Chem, 55 (1): (528-537). [PMID:22122563] [10.1021/jm201436k]
105. Harada K, Kubo H, Abe J, Haneta M, Conception A, Inoue S, Okada S, Nishioka K.. (2012) Discovery of potent and orally bioavailable 17β-hydroxysteroid dehydrogenase type 3 inhibitors.. Bioorg Med Chem, 20 (10): (3242-3254). [PMID:22512907] [10.1016/j.bmc.2012.03.052]
106. Wang P, Min J, Nwachukwu JC, Cavett V, Carlson KE, Guo P, Zhu M, Zheng Y, Dong C, Katzenellenbogen JA, Nettles KW, Zhou HB.. (2012) Identification and structure-activity relationships of a novel series of estrogen receptor ligands based on 7-thiabicyclo[2.2.1]hept-2-ene-7-oxide.. J Med Chem, 55 (5): (2324-2341). [PMID:22283328] [10.1021/jm201556r]
107. Hanson RN, Hua E, Hendricks JA, Labaree D, Hochberg RB.. (2012) Synthesis and evaluation of 11β-(4-substituted phenyl) estradiol analogs: transition from estrogen receptor agonists to antagonists.. Bioorg Med Chem, 20 (12): (3768-3780). [PMID:22608920] [10.1016/j.bmc.2012.04.041]
108. Henn C, Einspanier A, Marchais-Oberwinkler S, Frotscher M, Hartmann RW.. (2012) Lead optimization of 17β-HSD1 inhibitors of the (hydroxyphenyl)naphthol sulfonamide type for the treatment of endometriosis.. J Med Chem, 55 (7): (3307-3318). [PMID:22380653] [10.1021/jm201735j]
109. Caboni L, Kinsella GK, Blanco F, Fayne D, Jagoe WN, Carr M, Williams DC, Meegan MJ, Lloyd DG.. (2012) "True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer.. J Med Chem, 55 (4): (1635-1644). [PMID:22280402] [10.1021/jm201438f]
110. Chen T, Benmohamed R, Kim J, Smith K, Amante D, Morimoto RI, Kirsch DR, Ferrante RJ, Silverman RB.. (2012) ADME-guided design and synthesis of aryloxanyl pyrazolone derivatives to block mutant superoxide dismutase 1 (SOD1) cytotoxicity and protein aggregation: potential application for the treatment of amyotrophic lateral sclerosis.. J Med Chem, 55 (1): (515-527). [PMID:22191331] [10.1021/jm2014277]
111. Munuganti RS, Leblanc E, Axerio-Cilies P, Labriere C, Frewin K, Singh K, Hassona MD, Lack NA, Li H, Ban F, Tomlinson Guns E, Young R, Rennie PS, Cherkasov A.. (2013) Targeting the binding function 3 (BF3) site of the androgen receptor through virtual screening. 2. development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole derivatives.. J Med Chem, 56 (3): (1136-1148). [PMID:23301637] [10.1021/jm3015712]
112. Marchais-Oberwinkler S, Xu K, Wetzel M, Perspicace E, Negri M, Meyer A, Odermatt A, Möller G, Adamski J, Hartmann RW.. (2013) Structural optimization of 2,5-thiophene amides as highly potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors for the treatment of osteoporosis.. J Med Chem, 56 (1): (167-181). [PMID:23145773] [10.1021/jm3014053]
113. Min J, Wang P, Srinivasan S, Nwachukwu JC, Guo P, Huang M, Carlson KE, Katzenellenbogen JA, Nettles KW, Zhou HB.. (2013) Thiophene-core estrogen receptor ligands having superagonist activity.. J Med Chem, 56 (8): (3346-3366). [PMID:23586645] [10.1021/jm400157e]
114. Germain AR, Carmody LC, Nag PP, Morgan B, Verplank L, Fernandez C, Donckele E, Feng Y, Perez JR, Dandapani S, Palmer M, Lander ES, Gupta PB, Schreiber SL, Munoz B.. (2013) Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.. Bioorg Med Chem Lett, 23 (6): (1834-1838). [PMID:23403082] [10.1016/j.bmcl.2013.01.025]
115. Adam Hendricks J, Hanson RN, Amolins M, Mihelcic JM, Blagg BS.. (2013) Synthesis and preliminary evaluation steroidal antiestrogen-geldanamycin conjugates.. Bioorg Med Chem Lett, 23 (12): (3635-3639). [PMID:23648180] [10.1016/j.bmcl.2013.03.116]
116. Gryder BE, Rood MK, Johnson KA, Patil V, Raftery ED, Yao LP, Rice M, Azizi B, Doyle DF, Oyelere AK.. (2013) Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.. J Med Chem, 56 (14): (5782-5796). [PMID:23786452] [10.1021/jm400467w]
117. McCullough C, Neumann TS, Gone JR, He Z, Herrild C, Wondergem Nee Lukesh J, Pandey RK, Donaldson WA, Sem DS.. (2014) Probing the human estrogen receptor-α binding requirements for phenolic mono- and di-hydroxyl compounds: a combined synthesis, binding and docking study.. Bioorg Med Chem, 22 (1): (303-310). [PMID:24315190] [10.1016/j.bmc.2013.11.024]
118. Strong AL, Jiang Q, Zhang Q, Zheng S, Boue SM, Elliott S, Burow ME, Bunnell BA, Wang G.. (2014) Design, synthesis, and osteogenic activity of daidzein analogs on human mesenchymal stem cells.. ACS Med Chem Lett, 5 (2): (143-148). [PMID:24900787] [10.1021/ml400397k]
119. Sidhu PS, Nassif N, McCallum MM, Teske K, Feleke B, Yuan NY, Nandhikonda P, Cook JM, Singh RK, Bikle DD, Arnold LA.. (2014) Development of novel Vitamin D Receptor-Coactivator Inhibitors.. ACS Med Chem Lett, 5 (2): (199-204). [PMID:24799995] [10.1021/ml400462j]
120. Kajita D, Nakamura M, Matsumoto Y, Makishima M, Hashimoto Y.. (2014) Design and synthesis of silicon-containing steroid sulfatase inhibitors possessing pro-estrogen antagonistic character.. Bioorg Med Chem, 22 (7): (2244-2252). [PMID:24630694] [10.1016/j.bmc.2014.02.025]
121. Tang Z, Niu S, Liu F, Lao K, Miao J, Ji J, Wang X, Yan M, Zhang L, You Q, Xiao H, Xiang H.. (2014) Synthesis and biological evaluation of 2,3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.. Bioorg Med Chem Lett, 24 (9): (2129-2133). [PMID:24721727] [10.1016/j.bmcl.2014.03.042]
122. Maximov PY, Fernandes DJ, McDaniel RE, Myers CB, Curpan RF, Jordan VC.. (2014) Influence of the length and positioning of the antiestrogenic side chain of endoxifen and 4-hydroxytamoxifen on gene activation and growth of estrogen receptor positive cancer cells.. J Med Chem, 57 (11): (4569-4583). [PMID:24805199] [10.1021/jm500569h]
123. Perspicace E, Cozzoli L, Gargano EM, Hanke N, Carotti A, Hartmann RW, Marchais-Oberwinkler S.. (2014) Novel, potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors as potential therapeutics for osteoporosis with dual human and mouse activities.. Eur J Med Chem, 83 (317-337). [PMID:24974351] [10.1016/j.ejmech.2014.06.036]
124. Schroeder CE, Yao T, Sotsky J, Smith RA, Roy S, Chu YK, Guo H, Tower NA, Noah JW, McKellip S, Sosa M, Rasmussen L, Smith LH, White EL, Aubé J, Jonsson CB, Chung D, Golden JE.. (2014) Development of (E)-2-((1,4-dimethylpiperazin-2-ylidene)amino)-5-nitro-N-phenylbenzamide, ML336: Novel 2-amidinophenylbenzamides as potent inhibitors of venezuelan equine encephalitis virus.. J Med Chem, 57 (20): (8608-8621). [PMID:25244572] [10.1021/jm501203v]
125. Gargano EM, Perspicace E, Hanke N, Carotti A, Marchais-Oberwinkler S, Hartmann RW.. (2014) Metabolic stability optimization and metabolite identification of 2,5-thiophene amide 17β-hydroxysteroid dehydrogenase type 2 inhibitors.. Eur J Med Chem, 87 (203-219). [PMID:25259513] [10.1016/j.ejmech.2014.09.061]
126. Gege C, Schlüter T, Hoffmann T.. (2014) Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.. Bioorg Med Chem Lett, 24 (22): (5265-5267). [PMID:25305688] [10.1016/j.bmcl.2014.09.053]
127. Dabrota C, Asim M, Choueiri C, Gargaun A, Korobkov I, Butt A, Carlson KE, Katzenellenbogen JA, Wright JS, Durst T.. (2014) Synthesis and receptor binding in trans-CD ring-fused A-CD estrogens: comparison with the cis-fused isomers.. Bioorg Med Chem Lett, 24 (16): (3841-3844). [PMID:25027938] [10.1016/j.bmcl.2014.06.066]
128. Chen F, Liu J, Huang M, Hu M, Su Y, Zhang XK.. (2014) Identification of a New RXRα Antagonist Targeting the Coregulator-Binding Site.. ACS Med Chem Lett, 5 (7): (736-741). [PMID:25057340] [10.1021/ml5000405]
129. Li H, Ban F, Dalal K, Leblanc E, Frewin K, Ma D, Adomat H, Rennie PS, Cherkasov A.. (2014) Discovery of small-molecule inhibitors selectively targeting the DNA-binding domain of the human androgen receptor.. J Med Chem, 57 (15): (6458-6467). [PMID:25062331] [10.1021/jm500802j]
130. Ullrich T, Sasmal S, Boorgu V, Pasagadi S, Cheera S, Rajagopalan S, Bhumireddy A, Shashikumar D, Chelur S, Belliappa C, Pandit C, Krishnamurthy N, Mukherjee S, Ramanathan A, Ghadiyaram C, Ramachandra M, Santos PG, Lagu B, Bock MG, Perrone MH, Weiler S, Keller H.. (2014) 3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.. J Med Chem, 57 (17): (7396-7411). [PMID:25121964] [10.1021/jm5009049]
131. Paterni I, Bertini S, Granchi C, Tuccinardi T, Macchia M, Martinelli A, Caligiuri I, Toffoli G, Rizzolio F, Carlson KE, Katzenellenbogen BS, Katzenellenbogen JA, Minutolo F.. (2015) Highly selective salicylketoxime-based estrogen receptor β agonists display antiproliferative activities in a glioma model.. J Med Chem, 58 (3): (1184-1194). [PMID:25559213] [10.1021/jm501829f]
132. Lv W, Liu J, Skaar TC, Flockhart DA, Cushman M.. (2015) Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.. J Med Chem, 58 (6): (2623-2648). [PMID:25751283] [10.1021/jm501218e]
133. Yang C, Balsells J, Chu HD, Cox JM, Crespo A, Ma X, Contino L, Brown P, Gao S, Zamlynny B, Wiltsie J, Clemas J, Lisnock J, Gibson J, Zhou G, Garcia-Calvo M, Bateman TJ, Tong V, Xu L, Crook M, Sinclair P, Shen HC.. (2015) Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.. ACS Med Chem Lett, 6 (4): (461-465). [PMID:25941555] [10.1021/acsmedchemlett.5b00010]
134. Lai A, Kahraman M, Govek S, Nagasawa J, Bonnefous C, Julien J, Douglas K, Sensintaffar J, Lu N, Lee KJ, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Moon MJ, Joseph JD, Darimont B, Brigham D, Grillot K, Heyman R, Rix PJ, Hager JH, Smith ND.. (2015) Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.. J Med Chem, 58 (12): (4888-4904). [PMID:25879485] [10.1021/acs.jmedchem.5b00054]
135. Shoda T, Kato M, Harada R, Fujisato T, Okuhira K, Demizu Y, Inoue H, Naito M, Kurihara M.. (2015) Synthesis and evaluation of tamoxifen derivatives with a long alkyl side chain as selective estrogen receptor down-regulators.. Bioorg Med Chem, 23 (13): (3091-3096). [PMID:26003343] [10.1016/j.bmc.2015.05.002]
136. Tang C, Li C, Zhang S, Hu Z, Wu J, Dong C, Huang J, Zhou HB.. (2015) Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.. J Med Chem, 58 (11): (4550-4572). [PMID:25993269] [10.1021/acs.jmedchem.5b00099]
137. Hao XD, Chang J, Qin BY, Zhong C, Chu ZB, Huang J, Zhou WJ, Sun X.. (2015) Synthesis, estrogenic activity, and anti-osteoporosis effects in ovariectomized rats of resveratrol oligomer derivatives.. Eur J Med Chem, 102 (26-38). [PMID:26241875] [10.1016/j.ejmech.2015.07.042]
138. Thomas MP, Potter BV.. (2015) Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.. J Med Chem, 58 (19): (7634-7658). [PMID:25992880] [10.1021/acs.jmedchem.5b00386]
139. Mendoza-Sanchez R, Cotnoir-White D, Kulpa J, Jutras I, Pottel J, Moitessier N, Mader S, Gleason JL.. (2015) Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.. Bioorg Med Chem, 23 (24): (7597-7606). [PMID:26613635] [10.1016/j.bmc.2015.11.005]
140. Zhao C, Choi YH, Khadka DB, Jin Y, Lee KY, Cho WJ.. (2016) Design and synthesis of novel androgen receptor antagonists via molecular modeling.. Bioorg Med Chem, 24 (4): (789-801). [PMID:26780832] [10.1016/j.bmc.2015.12.047]
141. Xiong R, Patel HK, Gutgesell LM, Zhao J, Delgado-Rivera L, Pham TN, Zhao H, Carlson K, Martin T, Katzenellenbogen JA, Moore TW, Tonetti DA, Thatcher GR.. (2016) Selective Human Estrogen Receptor Partial Agonists (ShERPAs) for Tamoxifen-Resistant Breast Cancer.. J Med Chem, 59 (1): (219-237). [PMID:26681208] [10.1021/acs.jmedchem.5b01276]
142. Ahmed NS, Elghazawy NH, ElHady AK, Engel M, Hartmann RW, Abadi AH.. (2016) Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.. Eur J Med Chem, 112 (171-179). [PMID:26896706] [10.1016/j.ejmech.2016.02.026]
143. Sundén H, Schäfer A, Scheepstra M, Leysen S, Malo M, Ma JN, Burstein ES, Ottmann C, Brunsveld L, Olsson R.. (2016) Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation.. J Med Chem, 59 (3): (1232-1238). [PMID:26820900] [10.1021/acs.jmedchem.5b01702]
144. Shoda T, Kato M, Fujisato T, Misawa T, Demizu Y, Inoue H, Naito M, Kurihara M.. (2016) Synthesis and evaluation of raloxifene derivatives as a selective estrogen receptor down-regulator.. Bioorg Med Chem, 24 (13): (2914-2919). [PMID:27185013] [10.1016/j.bmc.2016.04.068]
145. Kelly PM, Bright SA, Fayne D, Pollock JK, Zisterer DM, Williams DC, Meegan MJ.. (2016) Synthesis, antiproliferative and pro-apoptotic activity of 2-phenylindoles.. Bioorg Med Chem, 24 (18): (4075-4099). [PMID:27407030] [10.1016/j.bmc.2016.06.050]
146. Tang Z, Wu C, Wang T, Lao K, Wang Y, Liu L, Muyaba M, Xu P, He C, Luo G, Qian Z, Niu S, Wang L, Wang Y, Xiao H, You Q, Xiang H.. (2016) Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents.. Eur J Med Chem, 118 (328-339). [PMID:27176944] [10.1016/j.ejmech.2016.04.029]
147. Zhao LM, Jin HS, Liu J, Skaar TC, Ipe J, Lv W, Flockhart DA, Cushman M.. (2016) A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptors α and β.. Bioorg Med Chem, 24 (21): (5400-5409). [PMID:27647367] [10.1016/j.bmc.2016.08.064]
148. Carpenter C, Sorenson RJ, Jin Y, Klossowski S, Cierpicki T, Gnegy M, Showalter HD.. (2016) Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.. Bioorg Med Chem, 24 (21): (5495-5504). [PMID:27647375] [10.1016/j.bmc.2016.09.002]
149. Yamada A, Kazui Y, Yoshioka H, Tanatani A, Mori S, Kagechika H, Fujii S.. (2016) Development of N-(4-Phenoxyphenyl)benzenesulfonamide Derivatives as Novel Nonsteroidal Progesterone Receptor Antagonists.. ACS Med Chem Lett, 7 (12): (1028-1033). [PMID:27994732] [10.1021/acsmedchemlett.6b00184]
150. Liu J, Zheng S, Guo S, Zhang C, Zhong Q, Zhang Q, Ma P, Skripnikova EV, Bratton MR, Wiese TE, Wang G.. (2017) Rational Design of a Boron-Modified Triphenylethylene (GLL398) as an Oral Selective Estrogen Receptor Downregulator.. ACS Med Chem Lett, 8 (1): (102-106). [PMID:28105283] [10.1021/acsmedchemlett.6b00410]
151. Abdelsamie AS, van Koppen CJ, Bey E, Salah M, Börger C, Siebenbürger L, Laschke MW, Menger MD, Frotscher M.. (2017) Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC50 for a proof-of-principle study.. Eur J Med Chem, 127 (944-957). [PMID:27852458] [10.1016/j.ejmech.2016.11.004]
152. Saravanan K, Elancheran R, Divakar S, Anand SA, Ramanathan M, Kotoky J, Lokanath NK, Kabilan S.. (2017) Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents.. Bioorg Med Chem Lett, 27 (5): (1199-1204). [PMID:28162857] [10.1016/j.bmcl.2017.01.065]
153. Xiong R, Zhao J, Gutgesell LM, Wang Y, Lee S, Karumudi B, Zhao H, Lu Y, Tonetti DA, Thatcher GR.. (2017) Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.. J Med Chem, 60 (4): (1325-1342). [PMID:28117994] [10.1021/acs.jmedchem.6b01355]
154. Zhang G, Liu S, Tan W, Verma R, Chen Y, Sun D, Huan Y, Jiang Q, Wang X, Wang N, Xu Y, Wong C, Shen Z, Deng R, Liu J, Zhang Y, Fang W.. (2017) Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists.. Eur J Med Chem, 129 (303-309). [PMID:28235703] [10.1016/j.ejmech.2017.02.037]
155. Burks HE, Abrams T, Kirby CA, Baird J, Fekete A, Hamann LG, Kim S, Lombardo F, Loo A, Lubicka D, Macchi K, McDonnell DP, Mishina Y, Norris JD, Nunez J, Saran C, Sun Y, Thomsen NM, Wang C, Wang J, Peukert S.. (2017) Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.. J Med Chem, 60 (7): (2790-2818). [PMID:28296398] [10.1021/acs.jmedchem.6b01468]
156. Min J, Guillen VS, Sharma A, Zhao Y, Ziegler Y, Gong P, Mayne CG, Srinivasan S, Kim SH, Carlson KE, Nettles KW, Katzenellenbogen BS, Katzenellenbogen JA.. (2017) Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.. J Med Chem, 60 (14): (6321-6336). [PMID:28657320] [10.1021/acs.jmedchem.7b00585]
157. Xie M, Zhao H, Liu Q, Zhu Y, Yin F, Liang Y, Jiang Y, Wang D, Hu K, Qin X, Wang Z, Wu Y, Xu N, Ye X, Wang T, Li Z.. (2017) Structural Basis of Inhibition of ERα-Coactivator Interaction by High-Affinity N-Terminus Isoaspartic Acid Tethered Helical Peptides.. J Med Chem, 60 (21): (8731-8740). [PMID:29045135] [10.1021/acs.jmedchem.7b00732]
158. Luo G, Chen M, Lyu W, Zhao R, Xu Q, You Q, Xiang H.. (2017) Design, synthesis, biological evaluation and molecular docking studies of novel 3-aryl-4-anilino-2H-chromen-2-one derivatives targeting ERα as anti-breast cancer agents.. Bioorg Med Chem Lett, 27 (12): (2668-2673). [PMID:28460819] [10.1016/j.bmcl.2017.04.029]
159. Piotrowski DW, Futatsugi K, Casimiro-Garcia A, Wei L, Sammons MF, Herr M, Jiao W, Lavergne SY, Coffey SB, Wright SW, Song K, Loria PM, Banker ME, Petersen DN, Bauman J.. (2018) Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.. J Med Chem, 61 (3): (1086-1097). [PMID:29300474] [10.1021/acs.jmedchem.7b01515]
160. Yang L, Hu Z, Luo J, Tang C, Zhang S, Ning W, Dong C, Huang J, Liu X, Zhou HB.. (2017) Dual functional small molecule fluorescent probes for image-guided estrogen receptor-specific targeting coupled potent antiproliferative potency for breast cancer therapy.. Bioorg Med Chem, 25 (13): (3531-3539). [PMID:28506582] [10.1016/j.bmc.2017.05.002]
161. Torikai K, Koga R, Liu X, Umehara K, Kitano T, Watanabe K, Oishi T, Noguchi H, Shimohigashi Y.. (2017) Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.. Bioorg Med Chem, 25 (20): (5216-5237). [PMID:28882502] [10.1016/j.bmc.2017.07.067]
162. Patch RJ, Huang H, Patel S, Cheung W, Xu G, Zhao BP, Beauchamp DA, Rentzeperis D, Geisler JG, Askari HB, Liu J, Kasturi J, Towers M, Gaul MD, Player MR.. (2017) Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.. Eur J Med Chem, 138 (830-853). [PMID:28735214] [10.1016/j.ejmech.2017.07.015]
163. Luo G, Li X, Zhang G, Wu C, Tang Z, Liu L, You Q, Xiang H.. (2017) Novel SERMs based on 3-aryl-4-aryloxy-2H-chromen-2-one skeleton - A possible way to dual ERα/VEGFR-2 ligands for treatment of breast cancer.. Eur J Med Chem, 140 (252-273). [PMID:28942113] [10.1016/j.ejmech.2017.09.015]
164. Abdel-Magid AF.. (2017) Selective Estrogen Receptor Degraders (SERDs): A Promising Treatment to Overcome Resistance to Endocrine Therapy in ERα-Positive Breast Cancer.. ACS Med Chem Lett, 8 (11): (1129-1131). [PMID:29152041] [10.1021/acsmedchemlett.7b00424]
165. Bergquist BL, Jefferson KG, Kintz HN, Barber AE, Yeagley AA.. (2018) Disconnecting the Estrogen Receptor Binding Properties and Antimicrobial Properties of Parabens through 3,5-Substitution.. ACS Med Chem Lett, 9 (1): (51-55). [PMID:29348811] [10.1021/acsmedchemlett.7b00431]
166. Carcache DA, Vulpetti A, Kallen J, Mattes H, Orain D, Stringer R, Vangrevelinghe E, Wolf RM, Kaupmann K, Ottl J, Dawson J, Cooke NG, Hoegenauer K, Billich A, Wagner J, Guntermann C, Hintermann S.. (2018) Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.. J Med Chem, 61 (15): (6724-6735). [PMID:29990434] [10.1021/acs.jmedchem.8b00529]
167. Misawa T, Fujisato T, Kanda Y, Ohoka N, Shoda T, Yorioka M, Makishima M, Sekino Y, Naito M, Demizu Y, Kurihara M.. (2017) Design and synthesis of novel selective estrogen receptor degradation inducers based on the diphenylheptane skeleton.. Medchemcomm, 8 (1): (239-246). [PMID:30108709] [10.1039/C6MD00553E]
168. Kuznetsov YV, Levina IS, Scherbakov AM, Andreeva OE, Fedyushkina IV, Dmitrenok AS, Shashkov AS, Zavarzin IV.. (2018) New estrogen receptor antagonists. 3,20-Dihydroxy-19-norpregna-1,3,5(10)-trienes: Synthesis, molecular modeling, and biological evaluation.. Eur J Med Chem, 143 (670-682). [PMID:29220789] [10.1016/j.ejmech.2017.11.042]
169. Singla R, Gupta KB, Upadhyay S, Dhiman M, Jaitak V.. (2018) Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-α).. Eur J Med Chem, 146 (206-219). [PMID:29407951] [10.1016/j.ejmech.2018.01.051]
170. Lee W, Ko KR, Kim HK, Lee DS, Nam IJ, Lim S, Kim S.. (2018) Dehydrodiconiferyl Alcohol Inhibits Osteoclast Differentiation and Ovariectomy-Induced Bone Loss through Acting as an Estrogen Receptor Agonist.. J Nat Prod, 81 (6): (1343-1356). [PMID:29869503] [10.1021/acs.jnatprod.7b00927]
171. Nagasawa J, Govek S, Kahraman M, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Lu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Maheu K, Heyman R, Rix PJ, Hager JH, Smith ND.. (2018) Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.. J Med Chem, 61 (17): (7917-7928). [PMID:30086626] [10.1021/acs.jmedchem.8b00921]
172. Rew Y, Du X, Eksterowicz J, Zhou H, Jahchan N, Zhu L, Yan X, Kawai H, McGee LR, Medina JC, Huang T, Chen C, Zavorotinskaya T, Sutimantanapi D, Waszczuk J, Jackson E, Huang E, Ye Q, Fantin VR, Sun D.. (2018) Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).. J Med Chem, 61 (17): (7767-7784). [PMID:30091920] [10.1021/acs.jmedchem.8b00743]
173. Vuorinen A, Engeli RT, Leugger S, Bachmann F, Akram M, Atanasov AG, Waltenberger B, Temml V, Stuppner H, Krenn L, Ateba SB, Njamen D, Davis RA, Odermatt A, Schuster D.. (2017) Potential Antiosteoporotic Natural Product Lead Compounds That Inhibit 17β-Hydroxysteroid Dehydrogenase Type 2.. J Nat Prod, 80 (4): (965-974). [PMID:28319389] [10.1021/acs.jnatprod.6b00950]
174. Teske KA, Bogart JW, Arnold LA.. (2018) Novel VDR antagonists based on the GW0742 scaffold.. Bioorg Med Chem Lett, 28 (3): (351-354). [PMID:29287957] [10.1016/j.bmcl.2017.12.041]
175. Singla R, Gupta KB, Upadhyay S, Dhiman M, Jaitak V.. (2018) Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators.. Bioorg Med Chem, 26 (1): (266-277). [PMID:29198894] [10.1016/j.bmc.2017.11.040]
176. Ning W, Hu Z, Tang C, Yang L, Zhang S, Dong C, Huang J, Zhou HB.. (2018) Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer.. J Med Chem, 61 (18): (8155-8173). [PMID:30053783] [10.1021/acs.jmedchem.8b00224]
177. O'Dea A, Sondergard C, Sweeney P, Arnatt CK.. (2018) A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.. ACS Med Chem Lett, 9 (9): (901-906). [PMID:30258538] [10.1021/acsmedchemlett.8b00212]
178. Liu L, Tang Z, Wu C, Li X, Huang A, Lu X, You Q, Xiang H.. (2018) Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents.. Bioorg Med Chem Lett, 28 (6): (1138-1142). [PMID:29482944] [10.1016/j.bmcl.2017.12.066]
179. Eto R, Misawa T, Noguchi-Yachide T, Ohoka N, Kurihara M, Naito M, Tanaka M, Demizu Y.. (2018) Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton.. Bioorg Med Chem, 26 (8): (1638-1642). [PMID:29525335] [10.1016/j.bmc.2018.02.010]
180. Luo G, Tang Z, Lao K, Li X, You Q, Xiang H.. (2018) Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity.. Eur J Med Chem, 150 (783-795). [PMID:29587221] [10.1016/j.ejmech.2018.03.018]
181. Qin W, Xie M, Qin X, Fang Q, Yin F, Li Z.. (2018) Recent advances in peptidomimetics antagonists targeting estrogen receptor α-coactivator interaction in cancer therapy.. Bioorg Med Chem Lett, 28 (17): (2827-2836). [PMID:30025900] [10.1016/j.bmcl.2018.05.062]
182. Hajirahimkhan A, Mbachu O, Simmler C, Ellis SG, Dong H, Nikolic D, Lankin DC, van Breemen RB, Chen SN, Pauli GF, Dietz BM, Bolton JL.. (2018) Estrogen Receptor (ER) Subtype Selectivity Identifies 8-Prenylapigenin as an ERβ Agonist from Glycyrrhiza inflata and Highlights the Importance of Chemical and Biological Authentication.. J Nat Prod, 81 (4): (966-975). [PMID:29641206] [10.1021/acs.jnatprod.7b01070]
183. Savić MP, Ajduković JJ, Plavša JJ, Bekić SS, Ćelić AS, Klisurić OR, Jakimov DS, Petri ET, Djurendić EA.. (2018) Evaluation of A-ring fused pyridine d-modified androstane derivatives for antiproliferative and aldo-keto reductase 1C3 inhibitory activity.. Medchemcomm, 9 (6): (969-981). [PMID:30108986] [10.1039/C8MD00077H]
184. Luo J, Hu Z, Xiao Y, Yang T, Dong C, Huang J, Zhou HB.. (2017) Rational design and optimization of selenophenes with basic side chains as novel potent selective estrogen receptor modulators (SERMs) for breast cancer therapy.. Medchemcomm, 8 (7): (1485-1497). [PMID:30108860] [10.1039/C7MD00163K]
185. Dalal K, Morin H, Ban F, Shepherd A, Fernandez M, Tam KJ, Li H, LeBlanc E, Lack N, Prinz H, Rennie PS, Cherkasov A.. (2018) Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor.. Eur J Med Chem, 157 (1164-1173). [PMID:30193215] [10.1016/j.ejmech.2018.08.059]
186. Hoegenauer K, Kallen J, Jiménez-Núñez E, Strang R, Ertl P, Cooke NG, Hintermann S, Voegtle M, Betschart C, McKay DJJ, Wagner J, Ottl J, Beerli C, Billich A, Dawson J, Kaupmann K, Streiff M, Gobeau N, Harlfinger S, Stringer R, Guntermann C.. (2019) Structure-Based and Property-Driven Optimization of N-Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors.. J Med Chem, 62 (23): (10816-10832). [PMID:31729873] [10.1021/acs.jmedchem.9b01291]
187. Li X, Wu C, Lin X, Cai X, Liu L, Luo G, You Q, Xiang H.. (2019) Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.. Eur J Med Chem, 161 (445-455). [PMID:30384047] [10.1016/j.ejmech.2018.10.045]
188. Kahraman M, Govek SP, Nagasawa JY, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Liu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Heyman R, Rix PJ, Hager JH, Smith ND.. (2019) Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927.. ACS Med Chem Lett, 10 (1): (50-55). [PMID:30655946] [10.1021/acsmedchemlett.8b00414]
189. Li Y, Zhang S, Zhang J, Hu Z, Xiao Y, Huang J, Dong C, Huang S, Zhou HB.. (2019) Exploring the PROTAC degron candidates: OBHSA with different side chains as novel selective estrogen receptor degraders (SERDs).. Eur J Med Chem, 172 (48-61). [PMID:30939353] [10.1016/j.ejmech.2019.03.058]
190. Lu Y, Gutgesell LM, Xiong R, Zhao J, Li Y, Rosales CI, Hollas M, Shen Z, Gordon-Blake J, Dye K, Wang Y, Lee S, Chen H, He D, Dubrovyskyii O, Zhao H, Huang F, Lasek AW, Tonetti DA, Thatcher GRJ.. (2019) Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.. J Med Chem, 62 (24): (11301-11323). [PMID:31746603] [10.1021/acs.jmedchem.9b01580]
191. Bechmann N, Kniess T, Pietzsch J.. (2019) Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index.. J Med Chem, 62 (14): (6525-6539). [PMID:31099568] [10.1021/acs.jmedchem.9b00171]
192. Hu Z, Li Y, Xie B, Ning W, Xiao Y, Huang Y, Zhao C, Huang J, Dong C, Zhou HB.. (2019) Novel class of 7-Oxabicyclo[2.2.1]heptene sulfonamides with long alkyl chains displaying improved estrogen receptor α degradation activity.. Eur J Med Chem, 182 (111605-111605). [PMID:31437778] [10.1016/j.ejmech.2019.111605]
193. Scott JS, Bailey A, Buttar D, Carbajo RJ, Curwen J, Davey PRJ, Davies RDM, Degorce SL, Donald C, Gangl E, Greenwood R, Groombridge SD, Johnson T, Lamont S, Lawson M, Lister A, Morrow CJ, Moss TA, Pink JH, Polanski R.. (2019) Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.. J Med Chem, 62 (3): (1593-1608). [PMID:30640465] [10.1021/acs.jmedchem.8b01837]
194. Passeri D, Carotti A, Pittol JMR, Ciaccioli G, Pellicciari R, van Mil SWC, Gioiello A.. (2019) Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.. Medchemcomm, 10 (8): (1412-1419). [PMID:31673308] [10.1039/C9MD00264B]
195. Nanjyo S, Ohgane K, Yoshioka H, Makishima M, Hashimoto Y, Noguchi-Yachide T.. (2019) Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.. Bioorg Med Chem, 27 (10): (1952-1961). [PMID:30940565] [10.1016/j.bmc.2019.03.042]
196. Park H, McEachon JD, Pollock JA.. (2019) Synthesis and characterization of hydrogen peroxide activated estrogen receptor beta ligands.. Bioorg Med Chem, 27 (10): (2075-2082). [PMID:30967304] [10.1016/j.bmc.2019.04.003]
197. Saha T, Makar S, Swetha R, Gutti G, Singh SK.. (2019) Estrogen signaling: An emanating therapeutic target for breast cancer treatment.. Eur J Med Chem, 177 (116-143). [PMID:31129450] [10.1016/j.ejmech.2019.05.023]
198. Hwang DJ, He Y, Ponnusamy S, Mohler ML, Thiyagarajan T, McEwan IJ, Narayanan R, Miller DD.. (2019) New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.. J Med Chem, 62 (2): (491-511). [PMID:30525603] [10.1021/acs.jmedchem.8b00973]
199. Kim J, Song J, Ji HD, Yoo EK, Lee JE, Lee SB, Oh JM, Lee S, Hwang JS, Yoon H, Kim DS, Lee SJ, Jeong M, Lee S, Kim KH, Choi HS, Lee SW, Park KG, Lee IK, Kim SH, Hwang H, Jeon YH, Chin J, Cho SJ.. (2019) Discovery of Potent, Selective, and Orally Bioavailable Estrogen-Related Receptor-γ Inverse Agonists To Restore the Sodium Iodide Symporter Function in Anaplastic Thyroid Cancer.. J Med Chem, 62 (4): (1837-1858). [PMID:30657313] [10.1021/acs.jmedchem.8b01296]
200. Zhang B, Kiefer JR, Blake RA, Chang JH, Hartman S, Ingalla ER, Kleinheinz T, Mody V, Nannini M, Ortwine DF, Ran Y, Sambrone A, Sampath D, Vinogradova M, Zhong Y, Nwachukwu JC, Nettles KW, Lai T, Liao J, Zheng X, Chen H, Wang X, Liang J.. (2019) Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.. Bioorg Med Chem Lett, 29 (7): (905-911). [PMID:30732944] [10.1016/j.bmcl.2019.01.036]
201. Liu J, Zheng S, Akerstrom VL, Yuan C, Ma Y, Zhong Q, Zhang C, Zhang Q, Guo S, Ma P, Skripnikova EV, Bratton MR, Pannuti A, Miele L, Wiese TE, Wang G.. (2016) Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD).. J Med Chem, 59 (17): (8134-8140). [PMID:27529700] [10.1021/acs.jmedchem.6b00753]
202. Liang J, Blake R, Chang J, Friedman LS, Goodacre S, Hartman S, Ingalla ER, Kiefer JR, Kleinheinz T, Labadie S, Li J, Lai KW, Liao J, Mody V, McLean N, Metcalfe C, Nannini M, Otwine D, Ran Y, Ray N, Roussel F, Sambrone A, Sampath D, Vinogradova M, Wai J, Wang T, Yeap K, Young A, Zbieg J, Zhang B, Zheng X, Zhong Y, Wang X.. (2020) Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.. ACS Med Chem Lett, 11 (6): (1342-1347). [PMID:32551022] [10.1021/acsmedchemlett.0c00224]
203. Scott JS,Moss TA,Balazs A,Barlaam B,Breed J,Carbajo RJ,Chiarparin E,Davey PRJ,Delpuech O,Fawell S,Fisher DI,Gagrica S,Gangl ET,Grebe T,Greenwood RD,Hande S,Hatoum-Mokdad H,Herlihy K,Hughes S,Hunt TA,Huynh H,Janbon SLM,Johnson T,Kavanagh S,Klinowska T,Lawson M,Lister AS,Marden S,McGinnity DF,Morrow CJ,Nissink JWM,O'Donovan DH,Peng B,Polanski R,Stead DS,Stokes S,Thakur K,Throner SR,Tucker MJ,Varnes J,Wang H,Wilson DM,Wu D,Wu Y,Yang B,Yang W. (2020) Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.. J Med Chem, 63 (23): (14530-14559). [PMID:32910656] [10.1021/acs.jmedchem.0c01163]
204. He Y,Hwang DJ,Ponnusamy S,Thiyagarajan T,Mohler ML,Narayanan R,Miller DD. (2020) Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer.. J Med Chem, 63 (21): (12642-12665). [PMID:33095584] [10.1021/acs.jmedchem.0c00943]
205. Pellicciari R,Passeri D,De Franco F,Mostarda S,Filipponi P,Colliva C,Gadaleta RM,Franco P,Carotti A,Macchiarulo A,Roda A,Moschetta A,Gioiello A. (2016) Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.. J Med Chem, 59 (19): (9201-9214). [PMID:27652492] [10.1021/acs.jmedchem.6b01126]
206. Kim J,Woo SY,Im CY,Yoo EK,Lee S,Kim HJ,Hwang HJ,Cho JH,Lee WS,Yoon H,Kim S,Kwon OB,Hwang H,Kim KH,Jeon JH,Singh TD,Kim SW,Hwang SY,Choi HS,Lee IK,Kim SH,Jeon YH,Chin J,Cho SJ. (2016) Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.. J Med Chem, 59 (22): (10209-10227). [PMID:27805390] [10.1021/acs.jmedchem.6b01204]
207. Knox A,Kalchschmid C,Schuster D,Gaggia F,Manzl C,Baecker D,Gust R. (2020) Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.. Eur J Med Chem, 192 (112191-112191). [PMID:32169784] [10.1016/j.ejmech.2020.112191]
208. Song D,Yu W,Ren Y,Zhu J,Wan C,Cai G,Guo J,Zhang W,Kong L. (2020) Discovery of bazedoxifene analogues targeting glycoprotein 130.. Eur J Med Chem, 199 (112375-112375). [PMID:32388278] [10.1016/j.ejmech.2020.112375]
209. Kuzminac IZ,Jakimov DS,Bekić SS,Ćelić AS,Marinović MA,Savić MP,Raičević VN,Kojić VV,Sakač MN. (2021) Synthesis and anticancer potential of novel 5,6-oxygenated and/or halogenated steroidal d-homo lactones.. Bioorg Med Chem, 30 (115935-115935). [PMID:33340938] [10.1016/j.bmc.2020.115935]
210. Dai,Y.; Yue,N.; Gong,J.; Liu,C.; Li,Q.; Zhou,J.; Huang,W.; Qian,H.. (2020) Development of cell-permeable peptide-based PROTACs targeting estrogen receptor α.. Eur J Med Chem, 187 (111967-111967). [PMID:31865016] [10.1016/j.ejmech.2019.111967]
211. Kim J,Hwang H,Yoon H,Lee JE,Oh JM,An H,Ji HD,Lee S,Cha E,Ma MJ,Kim DS,Lee SJ,Kadayat TM,Song J,Lee SW,Jeon JH,Park KG,Lee IK,Jeon YH,Chin J,Cho SJ. (2020) An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.. Eur J Med Chem, 205 (112501-112501). [PMID:32758860] [10.1016/j.ejmech.2020.112501]
212. Lin X,Xiang H,Luo G. (2020) Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance.. Eur J Med Chem, 206 (112689-112689). [PMID:32829249] [10.1016/j.ejmech.2020.112689]
213. Lv W,Liu J,Skaar TC,O'Neill E,Yu G,Flockhart DA,Cushman M. (2016) Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors.. J Med Chem, 59 (1.0): (157-170). [PMID:26704594] [10.1021/acs.jmedchem.5b01677]
214. Yonekubo S,Fushimi N,Miyagi T,Nakanishi O,Katsuno K,Ozawa M,Handa C,Furuya N,Muranaka H. (2016) Synthesis and structure-activity relationships of 1-benzylindane derivatives as selective agonists for estrogen receptor beta.. Bioorg Med Chem, 24 (22.0): (5895-5910). [PMID:27692995] [10.1016/j.bmc.2016.09.047]
215. He M,Ning W,Hu Z,Huang J,Dong C,Zhou HB. (2020) Design, synthesis and biological evaluation of novel dual-acting modulators targeting both estrogen receptor α (ERα) and lysine-specific demethylase 1 (LSD1) for treatment of breast cancer.. Eur J Med Chem, 195 (112281-112281). [PMID:32283297] [10.1016/j.ejmech.2020.112281]
216. Ing, N H NH, Beekman, J M JM, Tsai, S Y SY, Tsai, M J MJ and O'Malley, B W BW.. (1992) Members of the steroid hormone receptor superfamily interact with TFIIB (S300-II).. The Journal of biological chemistry, (5): [PMID:1517211]
217. Reese, J C JC and Katzenellenbogen, B S BS.. (1992) Characterization of a temperature-sensitive mutation in the hormone binding domain of the human estrogen receptor. Studies in cell extracts and intact cells and their implications for hormone-dependent transcriptional activation.. The Journal of biological chemistry, (15): [PMID:1577818]
218. Schwabe, J W JW, Neuhaus, D D and Rhodes, D D.. (1990) Solution structure of the DNA-binding domain of the oestrogen receptor.. Nature, (29): [PMID:2247153]
219. Tora, L L and 5 more authors.. (1989) The cloned human oestrogen receptor contains a mutation which alters its hormone binding properties.. The EMBO journal, [PMID:2792078]
220. Ravdin, P M PM, van Beurden, M M and Jordan, V C VC.. (1987) Estrogenic effects of phenolphthalein on human breast cancer cells in vitro.. Breast cancer research and treatment, [PMID:3620717]
221. Green, S S and 6 more authors.. (1986) Human oestrogen receptor cDNA: sequence, expression and homology to v-erb-A.. Nature, [PMID:3754034]
222. Joel, P B PB, Traish, A M AM and Lannigan, D A DA.. (1995) Estradiol and phorbol ester cause phosphorylation of serine 118 in the human estrogen receptor.. Molecular endocrinology (Baltimore, Md.), [PMID:7476978]
223. Arnold, S F SF, Obourn, J D JD, Jaffe, H H and Notides, A C AC.. (1995) Phosphorylation of the human estrogen receptor on tyrosine 537 in vivo and by src family tyrosine kinases in vitro.. Molecular endocrinology (Baltimore, Md.), [PMID:7539106]
224. Stein, B B and Yang, M X MX.. (1995) Repression of the interleukin-6 promoter by estrogen receptor is mediated by NF-kappa B and C/EBP beta.. Molecular and cellular biology, [PMID:7651415]
225. Arnold, S F SF, Obourn, J D JD, Jaffe, H H and Notides, A C AC.. (1994) Serine 167 is the major estradiol-induced phosphorylation site on the human estrogen receptor.. Molecular endocrinology (Baltimore, Md.), [PMID:7838153]
226. Pfeffer, U U, Fecarotta, E E, Castagnetta, L L and Vidali, G G.. (1993) Estrogen receptor variant messenger RNA lacking exon 4 in estrogen-responsive human breast cancer cell lines.. Cancer research, (15): [PMID:7916651]
227. Schwabe, J W JW, Chapman, L L, Finch, J T JT and Rhodes, D D.. (1993) The crystal structure of the estrogen receptor DNA-binding domain bound to DNA: how receptors discriminate between their response elements.. Cell, (5): [PMID:8221895]
228. Pink, J J JJ, Wu, S Q SQ, Wolf, D M DM, Bilimoria, M M MM and Jordan, V C VC.. (1996) A novel 80 kDa human estrogen receptor containing a duplication of exons 6 and 7.. Nucleic acids research, (1): [PMID:8600466]
229. McInerney, E M EM, Ince, B A BA, Shapiro, D J DJ and Katzenellenbogen, B S BS.. (1996) A transcriptionally active estrogen receptor mutant is a novel type of dominant negative inhibitor of estrogen action.. Molecular endocrinology (Baltimore, Md.), [PMID:8961262]
230. Anderson, T I TI and 13 more authors.. (1997) Screening for ESR mutations in breast and ovarian cancer patients.. Human mutation, [PMID:9195227]
231. Porter, W W, Saville, B B, Hoivik, D D and Safe, S S.. (1997) Functional synergy between the transcription factor Sp1 and the estrogen receptor.. Molecular endocrinology (Baltimore, Md.), [PMID:9328340]
232. Brzozowski, A M AM and 9 more authors.. (1997) Molecular basis of agonism and antagonism in the oestrogen receptor.. Nature, (16): [PMID:9338790]
233. Tanenbaum, D M DM, Wang, Y Y, Williams, S P SP and Sigler, P B PB.. (1998) Crystallographic comparison of the estrogen and progesterone receptor's ligand binding domains.. Proceedings of the National Academy of Sciences of the United States of America, (26): [PMID:9600906]
234. Maalouf, G J GJ, Xu, W W, Smith, T F TF and Mohr, S C SC.. (1998) Homology model for the ligand-binding domain of the human estrogen receptor.. Journal of biomolecular structure & dynamics, [PMID:9619507]
235. Rubino, D D and 9 more authors.. (1998) Characterization of Brx, a novel Dbl family member that modulates estrogen receptor action.. Oncogene, (14): [PMID:9627117]
236. Montano, M M MM and 5 more authors.. (1999) An estrogen receptor-selective coregulator that potentiates the effectiveness of antiestrogens and represses the activity of estrogens.. Proceedings of the National Academy of Sciences of the United States of America, (8): [PMID:10359819]
237. Hunter, D S DS and 5 more authors.. (1999) Estrogen receptor activation via activation function 2 predicts agonism of xenoestrogens in normal and neoplastic cells of the uterine myometrium.. Cancer research, (1): [PMID:10397250]
238. Rogatsky, I I, Trowbridge, J M JM and Garabedian, M J MJ.. (1999) Potentiation of human estrogen receptor alpha transcriptional activation through phosphorylation of serines 104 and 106 by the cyclin A-CDK2 complex.. The Journal of biological chemistry, (6): [PMID:10428798]
239. Schubert, E L EL, Lee, M K MK, Newman, B B and King, M C MC.. (1999) Single nucleotide polymorphisms (SNPs) in the estrogen receptor gene and breast cancer susceptibility.. The Journal of steroid biochemistry and molecular biology, [PMID:10619354]
240. Klinge, C M CM, Kaur, K K and Swanson, H I HI.. (2000) The aryl hydrocarbon receptor interacts with estrogen receptor alpha and orphan receptors COUP-TFI and ERRalpha1.. Archives of biochemistry and biophysics, (1): [PMID:10620335]
241. Saville, B B and 7 more authors.. (2000) Ligand-, cell-, and estrogen receptor subtype (alpha/beta)-dependent activation at GC-rich (Sp1) promoter elements.. The Journal of biological chemistry, (25): [PMID:10681512]
242. Stoner, M M and 8 more authors.. (2000) Inhibition of vascular endothelial growth factor expression in HEC1A endometrial cancer cells through interactions of estrogen receptor alpha and Sp3 proteins.. The Journal of biological chemistry, (28): [PMID:10816575]
243. Becherini, L L and 10 more authors.. (2000) Evidence of a linkage disequilibrium between polymorphisms in the human estrogen receptor alpha gene and their relationship to bone mass variation in postmenopausal Italian women.. Human molecular genetics, (12): [PMID:10942433]
244. Zhou, J J, Ng, S S, Adesanya-Famuiya, O O, Anderson, K K and Bondy, C A CA.. (2000) Testosterone inhibits estrogen-induced mammary epithelial proliferation and suppresses estrogen receptor expression.. FASEB journal : official publication of the Federation of American Societies for Experimental Biology, [PMID:10973921]
245. Tessier, C C and 6 more authors.. (2000) Estrogen receptors alpha and beta in rat decidua cells: cell-specific expression and differential regulation by steroid hormones and prolactin.. Endocrinology, [PMID:11014241]
246. Métivier, R R, Petit, F G FG, Valotaire, Y Y and Pakdel, F F.. (2000) Function of N-terminal transactivation domain of the estrogen receptor requires a potential alpha-helical structure and is negatively regulated by the A domain.. Molecular endocrinology (Baltimore, Md.), [PMID:11075817]
247. Benecke, A A, Chambon, P P and Gronemeyer, H H.. (2000) Synergy between estrogen receptor alpha activation functions AF1 and AF2 mediated by transcription intermediary factor TIF2.. EMBO reports, [PMID:11265755]
248. Vadlamudi, R K RK and 6 more authors.. (2001) Molecular cloning and characterization of PELP1, a novel human coregulator of estrogen receptor alpha.. The Journal of biological chemistry, (12): [PMID:11481323]
249. Maggiolini, M M and 6 more authors.. (2001) Estrogen receptor alpha mediates the proliferative but not the cytotoxic dose-dependent effects of two major phytoestrogens on human breast cancer cells.. Molecular pharmacology, [PMID:11502892]
250. Yahata, T T and 10 more authors.. (2001) Selective coactivation of estrogen-dependent transcription by CITED1 CBP/p300-binding protein.. Genes & development, (1): [PMID:11581164]
251. Métivier, R R, Penot, G G, Flouriot, G G and Pakdel, F F.. (2001) Synergism between ERalpha transactivation function 1 (AF-1) and AF-2 mediated by steroid receptor coactivator protein-1: requirement for the AF-1 alpha-helical core and for a direct interaction between the N- and C-terminal domains.. Molecular endocrinology (Baltimore, Md.), [PMID:11682626]
252. Locci, P P and 8 more authors.. (2001) Synthesis and secretion of transforming growth factor-beta1 by human desmoid fibroblast cell line and its modulation by toremifene.. Journal of interferon & cytokine research : the official journal of the International Society for Interferon and Cytokine Research, [PMID:11747628]
253. Norris, John D JD, Fan, Daju D, Sherk, Andrea A and McDonnell, Donald P DP.. (2002) A negative coregulator for the human ER.. Molecular endocrinology (Baltimore, Md.), [PMID:11875103]
254. Fabian, C J CJ and Kimler, B F BF.. Chemoprevention for high-risk women: tamoxifen and beyond.. The breast journal, [PMID:11906441]
255. and Dow, Karen Hassey KH.. (2002) Existing and emerging endocrine therapies for breast cancer.. Cancer nursing, [PMID:12080538]
256. Puddefoot, John R JR, Barker, Stewart S, Glover, Hilary R HR, Malouitre, Sylvanie D M SD and Vinson, Gavin P GP.. (2002) Non-competitive steroid inhibition of oestrogen receptor functions.. International journal of cancer, (1): [PMID:12209583]
257. Margeat, Emmanuel E and 5 more authors.. (2003) Ligands differentially modulate the protein interactions of the human estrogen receptors alpha and beta.. Journal of molecular biology, (7): [PMID:12547192]
258. Li, Lei L, Haynes, M Page MP and Bender, Jeffrey R JR.. (2003) Plasma membrane localization and function of the estrogen receptor alpha variant (ER46) in human endothelial cells.. Proceedings of the National Academy of Sciences of the United States of America, (15): [PMID:12682286]
259. Liu, Xuemei X and 7 more authors.. (2003) Antiestrogenic and DNA damaging effects induced by tamoxifen and toremifene metabolites.. Chemical research in toxicology, [PMID:12870885]
260. and Pasqualini, J R JR.. (2003) Differential effects of progestins on breast tissue enzymes.. Maturitas, (10): [PMID:14670645]
261. Ikeda, Kazuhiro K and 7 more authors.. (2004) Protein phosphatase 5 is a negative regulator of estrogen receptor-mediated transcription.. Molecular endocrinology (Baltimore, Md.), [PMID:14764652]
262. Barletta, Frank F and 5 more authors.. (2004) Characterization of the interactions of estrogen receptor and MNAR in the activation of cSrc.. Molecular endocrinology (Baltimore, Md.), [PMID:14963108]
263. Bu, Hengfu H and 7 more authors.. (2004) ERBP, a novel estrogen receptor binding protein enhancing the activity of estrogen receptor.. Biochemical and biophysical research communications, (23): [PMID:15047147]
264. Mérot, Yohann Y and 8 more authors.. (2004) The relative contribution exerted by AF-1 and AF-2 transactivation functions in estrogen receptor alpha transcriptional activity depends upon the differentiation stage of the cell.. The Journal of biological chemistry, (18): [PMID:15078875]
265. Jung, Joohee J, Ishida, Kunie K and Nishihara, Tsutomu T.. (2004) Anti-estrogenic activity of fifty chemicals evaluated by in vitro assays.. Life sciences, (7): [PMID:15081572]
266. Damdimopoulos, Anastasios E AE, Miranda-Vizuete, Antonio A, Treuter, Eckardt E, Gustafsson, Jan-Ake JA and Spyrou, Giannis G.. (2004) An alternative splicing variant of the selenoprotein thioredoxin reductase is a modulator of estrogen signaling.. The Journal of biological chemistry, (10): [PMID:15199063]
267. del Río, Beatriz B and 5 more authors.. (2004) Melatonin, an endogenous-specific inhibitor of estrogen receptor alpha via calmodulin.. The Journal of biological chemistry, (10): [PMID:15229223]
268. Rayala, Suresh K SK and 5 more authors.. (2005) Functional regulation of oestrogen receptor pathway by the dynein light chain 1.. EMBO reports, [PMID:15891768]
269. Wittmann, Bryan M BM, Fujinaga, Koh K, Deng, Huayun H, Ogba, Ndiya N and Montano, Monica M MM.. (2005) The breast cell growth inhibitor, estrogen down regulated gene 1, modulates a novel functional interaction between estrogen receptor alpha and transcriptional elongation factor cyclin T1.. Oncogene, (25): [PMID:15940264]
270. Vereide, Anne Beate AB, Kaino, Turid T, Sager, Georg G, Arnes, Marit M and Ørbo, Anne A.. (2006) Effect of levonorgestrel IUD and oral medroxyprogesterone acetate on glandular and stromal progesterone receptors (PRA and PRB), and estrogen receptors (ER-alpha and ER-beta) in human endometrial hyperplasia.. Gynecologic oncology, [PMID:16325240]
271. Wei, Xiaolong X, Xu, Hai H and Kufe, Donald D.. (2006) MUC1 oncoprotein stabilizes and activates estrogen receptor alpha.. Molecular cell, (20): [PMID:16427018]
272. Ariazi, Eric A EA, Ariazi, Jennifer L JL, Cordera, Fernando F and Jordan, V Craig VC.. (2006) Estrogen receptors as therapeutic targets in breast cancer.. Current topics in medicinal chemistry, [PMID:16515478]
273. Farooqui, Mariya M and 5 more authors.. (2006) Naloxone acts as an antagonist of estrogen receptor activity in MCF-7 cells.. Molecular cancer therapeutics, [PMID:16546975]
274. Mo, Rigen R, Rao, Sambasiva M SM and Zhu, Yi-Jun YJ.. (2006) Identification of the MLL2 complex as a coactivator for estrogen receptor alpha.. The Journal of biological chemistry, (9): [PMID:16603732]
275. Gururaj, Anupama E AE and 9 more authors.. (2006) MTA1, a transcriptional activator of breast cancer amplified sequence 3.. Proceedings of the National Academy of Sciences of the United States of America, (25): [PMID:16617102]
276. Rayala, Suresh K SK and 8 more authors.. (2006) Essential role of KIBRA in co-activator function of dynein light chain 1 in mammalian cells.. The Journal of biological chemistry, (14): [PMID:16684779]
277. Dhananjayan, Sarath C SC and 7 more authors.. (2006) WW domain binding protein-2, an E6-associated protein interacting protein, acts as a coactivator of estrogen and progesterone receptors.. Molecular endocrinology (Baltimore, Md.), [PMID:16772533]
278. Hou, Ning Ning NN, Zhu, Yi Min YM and Huang, He Feng HF.. (2006) [The expression of estrogen receptor alpha and beta in the intervention of different estrogens in rat bone metabolism].. Fen zi xi bao sheng wu xue bao = Journal of molecular cell biology, [PMID:16955786]
279. Luboshits, G G and Benayahu, D D.. (2007) MS-KIF18A, a kinesin, is associated with estrogen receptor.. Journal of cellular biochemistry, (15): [PMID:17006958]
280. Manavathi, Bramanandam B, Acconcia, Filippo F, Rayala, Suresh K SK and Kumar, Rakesh R.. (2006) An inherent role of microtubule network in the action of nuclear receptor.. Proceedings of the National Academy of Sciences of the United States of America, (24): [PMID:17043237]
281. Lopez-Garcia, Jorge J and 11 more authors.. (2006) ZNF366 is an estrogen receptor corepressor that acts through CtBP and histone deacetylases.. Nucleic acids research, [PMID:17085477]
282. Lessey, Bruce A BA, Palomino, Wilder A WA, Apparao, K B C KB, Young, Steven L SL and Lininger, Ruth A RA.. (2006) Estrogen receptor-alpha (ER-alpha) and defects in uterine receptivity in women.. Reproductive biology and endocrinology : RB&E, [PMID:17118173]
283. Garcia-Segura, Luis M LM, Sanz, Amaya A and Mendez, Pablo P.. (2006) Cross-talk between IGF-I and estradiol in the brain: focus on neuroprotection.. Neuroendocrinology, [PMID:17124377]
284. Brama, Marina M and 10 more authors.. (2007) Cadmium induces mitogenic signaling in breast cancer cell by an ERalpha-dependent mechanism.. Molecular and cellular endocrinology, (29): [PMID:17125913]
285. Yuri, Takashi T, Tsukamoto, Reiko R, Uehara, Norihisa N, Matsuoka, Yoichiro Y and Tsubura, Airo A.. Effects of different durations of estrogen and progesterone treatment on development of N-methyl-N-nitrosourea-induced mammary carcinomas in female Lewis rats.. In vivo (Athens, Greece), [PMID:17203775]
286. Chanock, Stephen J SJ and 11 more authors.. (2007) Somatic sequence alterations in twenty-one genes selected by expression profile analysis of breast carcinomas.. Breast cancer research : BCR, [PMID:17224074]
287. Wang, Jia-yu JY, Xu, Bing-he BH, Tian, Li-jun LJ and Wang, Yan Y.. (2006) [Clinical characteristics and potential prognostic factors of breast cancer patients with liver metastases].. Zhonghua zhong liu za zhi [Chinese journal of oncology], [PMID:17236558]
288. Dixon, Alexis A, Wells, Corinne C CC, Singh, Sandhya S, Babayan, Regina R and Maric, Christine C.. (2007) Renoprotective effects of a selective estrogen receptor modulator, raloxifene, in an animal model of diabetic nephropathy.. American journal of nephrology, [PMID:17308373]
289. Yan, Jun J and 5 more authors.. (2007) Ubiquitin-interaction motifs of RAP80 are critical in its regulation of estrogen receptor alpha.. Nucleic acids research, [PMID:17311814]
290. Baron, Sylvain S and 5 more authors.. (2007) Estrogen receptor alpha and the activating protein-1 complex cooperate during insulin-like growth factor-I-induced transcriptional activation of the pS2/TFF1 gene.. The Journal of biological chemistry, (20): [PMID:17317669]
291. Montero Girard, Guadalupe G and 11 more authors.. (2007) Association of estrogen receptor-alpha and progesterone receptor A expression with hormonal mammary carcinogenesis: role of the host microenvironment.. Breast cancer research : BCR, [PMID:17341305]
292. Ghebeh, Hazem H and 6 more authors.. (2007) Expression of B7-H1 in breast cancer patients is strongly associated with high proliferative Ki-67-expressing tumor cells.. International journal of cancer, (15): [PMID:17415709]
293. Gururaj, Anupama E AE, Peng, Shaohua S, Vadlamudi, Ratna K RK and Kumar, Rakesh R.. (2007) Estrogen induces expression of BCAS3, a novel estrogen receptor-alpha coactivator, through proline-, glutamic acid-, and leucine-rich protein-1 (PELP1).. Molecular endocrinology (Baltimore, Md.), [PMID:17505058]
294. Meyer, Rene R, Wolf, Siegmund S SS and Obendorf, Maik M.. (2007) PRMT2, a member of the protein arginine methyltransferase family, is a coactivator of the androgen receptor.. The Journal of steroid biochemistry and molecular biology, [PMID:17587566]
295. Revankar, Chetana M CM and 8 more authors.. (2007) Synthetic estrogen derivatives demonstrate the functionality of intracellular GPR30.. ACS chemical biology, (17): [PMID:17655271]
296. Eriksson, Maria M and 6 more authors.. (2007) The NMDAR subunit NR3A interacts with microtubule-associated protein 1S in the brain.. Biochemical and biophysical research communications, (14): [PMID:17658481]
297. Han, W-D WD and 11 more authors.. (2007) Estrogenically regulated LRP16 interacts with estrogen receptor alpha and enhances the receptor's transcriptional activity.. Endocrine-related cancer, [PMID:17914104]
298. Molli, P R PR, Singh, R R RR, Lee, S W SW and Kumar, R R.. (2008) MTA1-mediated transcriptional repression of BRCA1 tumor suppressor gene.. Oncogene, (27): [PMID:17922032]
299. Nettles, Kendall W KW and 5 more authors.. (2008) CBP Is a dosage-dependent regulator of nuclear factor-kappaB suppression by the estrogen receptor.. Molecular endocrinology (Baltimore, Md.), [PMID:17932106]
300. Lambertini, Elisabetta E and 5 more authors.. (2008) ERalpha and AP-1 interact in vivo with a specific sequence of the F promoter of the human ERalpha gene in osteoblasts.. Journal of cellular physiology, [PMID:18247370]
301. Chen, Ming M, Ni, Jing J, Zhang, Yong Y, Muyan, Mesut M and Yeh, Shuyuan S.. (2008) ERAP75 functions as a coactivator to enhance estrogen receptor alpha transactivation in prostate stromal cells.. The Prostate, (1): [PMID:18563714]
302. Maru, Benit S BS and 5 more authors.. (2009) Potential use of an estrogen-glucocorticoid receptor chimera as a drug screen for tissue selective estrogenic activity.. Bone, [PMID:18976723]
303. Amadasi, Alessio; Mozzarelli, Andrea; Meda, Clara; Maggi, Adriana and Cozzini, Pietro.. (2009) Identification of xenoestrogens in food additives by an integrated in silico and in vitro approach.. Chemical research in toxicology, [PMID:19063592]
304. Jayaraman, A and Pike, C J.. (2009) Progesterone attenuates oestrogen neuroprotection via downregulation of oestrogen receptor expression in cultured neurones.. Journal of neuroendocrinology, [PMID:19094096]
305. Johnsen, Steven A SA and 13 more authors.. (2009) Regulation of estrogen-dependent transcription by the LIM cofactors CLIM and RLIM in breast cancer.. Cancer research, (1): [PMID:19117995]
306. Giamas, Georgios G and 9 more authors.. (2009) CK1delta modulates the transcriptional activity of ERalpha via AIB1 in an estrogen-dependent manner and regulates ERalpha-AIB1 interactions.. Nucleic acids research, [PMID:19339517]
307. Gionet, Nathalie N, Jansson, Deidre D, Mader, Sylvie S and Pratt, M A Christine MA.. (2009) NF-kappaB and estrogen receptor alpha interactions: Differential function in estrogen receptor-negative and -positive hormone-independent breast cancer cells.. Journal of cellular biochemistry, (1): [PMID:19350539]
308. Stanisić, Vladimir V, Malovannaya, Anna A, Qin, Jun J, Lonard, David M DM and O'Malley, Bert W BW.. (2009) OTU Domain-containing ubiquitin aldehyde-binding protein 1 (OTUB1) deubiquitinates estrogen receptor (ER) alpha and affects ERalpha transcriptional activity.. The Journal of biological chemistry, (12): [PMID:19383985]
309. Lappano, Rosamaria R and 12 more authors.. (2009) Structure-activity relationships of resveratrol and derivatives in breast cancer cells.. Molecular nutrition & food research, [PMID:19496085]
310. Zusev, Margalit and Benayahu, Dafna.. (2009) The regulation of MS-KIF18A expression and cross talk with estrogen receptor.. PloS one, (28): [PMID:19636373]
311. Li, Tingting T and 5 more authors.. (2009) SH2D4A regulates cell proliferation via the ERalpha/PLC-gamma/PKC pathway.. BMB reports, (31): [PMID:19712589]
312. Wortham, N C NC and 12 more authors.. (2009) The DEAD-box protein p72 regulates ERalpha-/oestrogen-dependent transcription and cell growth, and is associated with improved survival in ERalpha-positive breast cancer.. Oncogene, (19): [PMID:19718048]
313. Vivacqua, Adele A and 8 more authors.. (2009) G protein-coupled receptor 30 expression is up-regulated by EGF and TGF alpha in estrogen receptor alpha-positive cancer cells.. Molecular endocrinology (Baltimore, Md.), [PMID:19749156]
314. Bombail, Vincent V, Collins, Frances F, Brown, Pamela P and Saunders, Philippa T K PT.. (2010) Modulation of ER alpha transcriptional activity by the orphan nuclear receptor ERR beta and evidence for differential effects of long- and short-form splice variants.. Molecular and cellular endocrinology, (15): [PMID:19755138]
315. Brown, Julie J, Farquhar, Cindy C, Beck, James J, Boothroyd, Clare C and Hughes, Edward E.. (2009) Clomiphene and anti-oestrogens for ovulation induction in PCOS.. The Cochrane database of systematic reviews, (7): [PMID:19821295]
316. and Dang, ZhiChao Z.. (2010) Comparison of relative binding affinities to fish and mammalian estrogen receptors: the regulatory implications.. Toxicology letters, (15): [PMID:19913605]
317. Koyama, Satoshi S and 12 more authors.. (2010) Repression of estrogen receptor beta function by putative tumor suppressor DBC1.. Biochemical and biophysical research communications, (12): [PMID:20074560]
318. Guyot, Romain R, Vincent, Séverine S, Bertin, Julie J, Samarut, Jacques J and Ravel-Chapuis, Patrick P.. (2010) The transforming acidic coiled coil (TACC1) protein modulates the transcriptional activity of the nuclear receptors TR and RAR.. BMC molecular biology, (15): [PMID:20078863]
319. Dulos, John J and 7 more authors.. (2010) Suppression of the inflammatory response in experimental arthritis is mediated via estrogen receptor alpha but not estrogen receptor beta.. Arthritis research & therapy, [PMID:20497523]
320. Cyrus, Kedra K and 5 more authors.. (2010) Jostling for position: optimizing linker location in the design of estrogen receptor-targeting PROTACs.. ChemMedChem, (5): [PMID:20512796]
321. Pradhan, Madhumita M, Bembinster, Leslie A LA, Baumgarten, Sarah C SC and Frasor, Jonna J.. (2010) Proinflammatory cytokines enhance estrogen-dependent expression of the multidrug transporter gene ABCG2 through estrogen receptor and NF{kappa}B cooperativity at adjacent response elements.. The Journal of biological chemistry, (8): [PMID:20705611]
322. Dong, Xue-Yuan XY and 6 more authors.. (2010) ATBF1 inhibits estrogen receptor (ER) function by selectively competing with AIB1 for binding to the ER in ER-positive breast cancer cells.. The Journal of biological chemistry, (22): [PMID:20720010]
323. Shyu, Conrad; Cavileer, Timothy D; Nagler, James J and Ytreberg, F Marty.. (2011) Computational estimation of rainbow trout estrogen receptor binding affinities for environmental estrogens.. Toxicology and applied pharmacology, (1): [PMID:21075131]
324. Park, Yeomyung Y and 7 more authors.. (2011) Mammalian MST2 kinase and human Salvador activate and reduce estrogen receptor alpha in the absence of ligand.. Journal of molecular medicine (Berlin, Germany), [PMID:21104395]
325. Heldring, Nina N and 6 more authors.. (2011) Multiple sequence-specific DNA-binding proteins mediate estrogen receptor signaling through a tethering pathway.. Molecular endocrinology (Baltimore, Md.), [PMID:21330404]
326. Giamas, Georgios G and 16 more authors.. (2011) Kinome screening for regulators of the estrogen receptor identifies LMTK3 as a new therapeutic target in breast cancer.. Nature medicine, [PMID:21602804]
327. Kim, Kyung Hee KH, Toomre, Derek D and Bender, Jeffrey R JR.. (2011) Splice isoform estrogen receptors as integral transmembrane proteins.. Molecular biology of the cell, [PMID:21937726]
328. Pedram, Ali A, Razandi, Mahnaz M, Deschenes, Robert J RJ and Levin, Ellis R ER.. (2012) DHHC-7 and -21 are palmitoylacyltransferases for sex steroid receptors.. Molecular biology of the cell, [PMID:22031296]
329. Pradhan, Madhumita M, Baumgarten, Sarah C SC, Bembinster, Leslie A LA and Frasor, Jonna J.. (2012) CBP mediates NF-κB-dependent histone acetylation and estrogen receptor recruitment to an estrogen response element in the BIRC3 promoter.. Molecular and cellular biology, [PMID:22083956]
330. Li, S S and 9 more authors.. (2013) CLOCK is a substrate of SUMO and sumoylation of CLOCK upregulates the transcriptional activity of estrogen receptor-α.. Oncogene, (10): [PMID:23160374]
331. Feng, Yuxin Y and 8 more authors.. (2013) DNA homologous recombination factor SFR1 physically and functionally interacts with estrogen receptor alpha.. PloS one, [PMID:23874500]
332. Banerjee, Monimoy M, Robbins, Delira D and Chen, Taosheng T.. (2013) Modulation of xenobiotic receptors by steroids.. Molecules (Basel, Switzerland), (24): [PMID:23884115]
333. Poulard, Coralie C, Rambaud, Juliette J, Hussein, Nader N, Corbo, Laura L and Le Romancer, Muriel M.. (2014) JMJD6 regulates ERα methylation on arginine.. PloS one, [PMID:24498420]
334. Paterni, Ilaria I, Granchi, Carlotta C, Katzenellenbogen, John A JA and Minutolo, Filippo F.. (2014) Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential.. Steroids, [PMID:24971815]
335. Yoo, Hee Min HM and 14 more authors.. (2014) Modification of ASC1 by UFM1 is crucial for ERα transactivation and breast cancer development.. Molecular cell, (23): [PMID:25219498]
336. Paris, Françoise F, Balaguer, Patrick P, Rimbault, Frédéric F, Gaspari, Laura L and Sultan, Charles C.. (2015) Molecular action of norgestimate: new developments.. Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology, [PMID:25970022]
337. Mohammed, Hisham H and 24 more authors.. (2015) Progesterone receptor modulates ERα action in breast cancer.. Nature, (16): [PMID:26153859]
338. Ronghe, Amruta A and 7 more authors.. (2016) 4-(E)-{(p-tolylimino)-methylbenzene-1,2-diol}, 1 a novel resveratrol analog, differentially regulates estrogen receptors α and β in breast cancer cells.. Toxicology and applied pharmacology, (15): [PMID:26970359]
339. Bernard, Valérie V and 11 more authors.. (2017) Familial Multiplicity of Estrogen Insensitivity Associated With a Loss-of-Function ESR1 Mutation.. The Journal of clinical endocrinology and metabolism, (1): [PMID:27754803]
340. Britschgi, Adrian A and 20 more authors.. (2017) The Hippo kinases LATS1 and 2 control human breast cell fate via crosstalk with ERα.. Nature, (26): [PMID:28068668]
341. Tressler, Caitlin M and Zondlo, Neal J.. (2017) Perfluoro-tert-butyl Homoserine Is a Helix-Promoting, Highly Fluorinated, NMR-Sensitive Aliphatic Amino Acid: Detection of the Estrogen Receptor·Coactivator Protein-Protein Interaction by 19F NMR.. Biochemistry, (28): [PMID:28165218]
342. Benoit, Thibaut and 10 more authors.. (2017) Estetrol, a Fetal Selective Estrogen Receptor Modulator, Acts on the Vagina of Mice through Nuclear Estrogen Receptor α Activation.. The American journal of pathology, [PMID:28827141]

溶液计算器

摩尔浓度计算器

计算溶液所需的质量、体积或浓度。

质量

浓度

体积

分子量

g/mol

稀释计算器

计算配制储备溶液所需的稀释度。

浓度1（C1）

体积 1 (V1)

浓度 2 (C2)

体积 2 (V2)

复溶计算器

复溶计算器允许您快速计算试剂的体积，以复溶小瓶。只需输入试剂的质量和目标浓度，计算器将确定其余部分。

体积（添加到小瓶中）

质量（小瓶）

所需的复溶浓度

货号 (SKU)	包装规格	是否现货
rp175926-10μg (试用装) 申请此免费试用装（?）作为尊贵的客户，您每年可免费申请一次试用装产品，尽享探索与享受！	10μg	现货
rp175926-100μg	100μg	现货
rp175926-1mg	1mg	期货

Recombinant Human Estrogen Receptor alpha Protein

库存信息

库存信息

库存信息

基本描述

AI解读

图片

产品规格参数

技术规格说明书

质检证书（CoA,COO,BSE/TSE 和分析图谱)

相关文档

参考文献

溶液计算器

摩尔浓度计算器

稀释计算器

复溶计算器

相关技术文章