JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2024
·
IF 1.5
Xu Xiang,Mao Yiyin,Zhou Peng,Wu Yujing,Liu Yaling,Wang Hongyong,Lu Chunxiong,Zou Pei
In this study, a 99m Tc-labeled small molecule imaging probe [ 99m Tc]Tc-PG3C-CBM for PD-L1 imaging was designed. It showed a radiochemical yield of > 97% and good in vitro stability. Uptake in A375-hPD-L1 cells (17.07 ± 1.40%) was 4.5 times higher than in A375 cells (3.81 ± 0.19%). The probe demonstrated moderate PD-L1 affinity (K D : 11.6 ± 2.57 nM; IC 50 : 59.2 ± 2.40 nM). Additionally, SPECT/CT imaging and biodistribution results indicated that [ 99m Tc]Tc-PG3C-CBM was mainly metabolized by the liver and showed some accumulation at the tumor site. These results suggest that [ 99m Tc]Tc-PG3C-CBM could potentially target PD-L1 at tumor sites.
研究领域:
核医学
·
分子影像学
·
肿瘤学
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DOI
高影响因子
JOURNAL OF MEDICINAL CHEMISTRY
·
2025
·
IF 6.8
Zuojie Li,Lina Diao,Peiwen Han,Qingna Xiao,Dajie Ding,Junhong Feng,Jianyong Jiang,Junbo Zhang
Radiolabeled human epidermal growth factor receptor 2 (HER2) tracers are important tools for the accurate clinical diagnosis and treatment of HER2-positive tumors. The aim of this study was to investigate the potential of small molecule inhibitors (lapatinib) as target groups for novel radiotracers targeting HER2. Twelve stable radiotracers were prepared by chelation with different coligands. The relationships between the linker and the combination of coligands with pharmacodynamics were systematically evaluated. [99mTc]Tc-Lapa-HYNIC-TPPTS exhibits the most favorable pharmacokinetic properties, as it can stably bind to the active pocket of the HER2 protein. Both in vitro and in vivo studies demonstrated its high targeting specificity toward HER2. SPECT images of [99mTc]Tc-Lapa-HYNIC-TPPTS in HER2-positive model mice revealed that it can effectively locate tumors. This study is the first attempt at a 99mTc-labeled small-molecule inhibitor tracer targeting HER2, showing great potential for applications in the diagnosis of HER2-positive cancers.
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DOI
PubMed
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2016
·Vol. 311
·期 3
·1697-1708
·
IF 0.983
Xie Qinghua,Li Xia,Wang Guanquan,Hou Xuan,Wang Yujun,Yu Hongbo,Qu Changfa,Luo Shunzhong,Cui Yali,Xia Chuanqin,Wang Ruibing
Here we reported the radiolabeling and evaluation of a novel 131 I-radiolabeled quercetin for the treatment of dedifferentiated thyroid cancers. The human thyroid cancer cell lines (FTC-133, TT and DRO) experienced much higher uptake of 131 I-quercetin as compared to the free 131 I. And the proliferation inhibition rate of 131 I-quercetin on in vitro DRO cell line was 86.87 ± 7.15%. Biodistribution and SPECT analysis demonstrated that the injected radioactivity mainly accumulated in tumors. The tumor volume in the treatment group was dramatically inhibited in comparison with the control group.
研究领域:
核医学
·
肿瘤学
·
药理学
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产品关联
DOI
高影响因子
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY
·
2023
·
IF 5.4
Kaili Qin,Suling Xin,Gang Li,Kuncheng Zhou,Rongbin Pan,Shuying Chen,Tianming Tao,Changsheng Li,Ji Tao,Ray P.S. Han,Yuanbiao Tu
Cancer molecular imaging using specific probes designed to identify target proteins in cancer is a powerful tool to guide therapeutic selection, patient management, and follow-up. We demonstrated that icatibant may be used as a targeting probe for the significantly upregulated bradykinin B2R in colorectal cancer (CRC). Icatibant-based probes with high affinity towards bradykinin B2R were identified. The near-infrared (NIR) fluorescent dye conjugate MPA-PEG 3 -k-Icatibant and radioconjugate [ 99m Tc]Tc-HYNIC-PEG 4 -Icatibant exhibited favourable selective and specific uptake in tumours when the subcutaneous and orthotopic colorectal tumour-bearing mouse models were imaged using NIR fluorescence imaging and Single-Photon Emission Computed Tomography–Computed Tomography (SPECT-CT), respectively. The tracer of [ 99m Tc]Tc-HYNIC-PEG 4 -Icatibant accumulated in tumours according to biodistribution studies and peaked at 4 h with an uptake value of 3.41 ± 0.27%ID/g in HT29 tumour-bearing nude mice following intravenous injection (i.v.). The tumour-to-colorectal signal ratios were 5.03 ± 0.37, 15.45 ± 0.32, 13.58 ± 1.19 and 11.33 ± 1.73 1, 2, 4 and 6 h after tail-veil injection, respectively. Overall, in the wake of rapid and precise tumour delineation and penetration characteristics, icatibant-based probes represent promising high-contrast molecular imaging probes for the detection of bradykinin B2R.
研究领域:
肿瘤学
·
分子成像
·
癌症生物学
·
放射学
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产品关联
DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2021
·
IF 4.939
Huan Ma,Feize Li,Guohua Shen,Huawei Cai,Weihao Liu,Tu Lan,Yuanyou Yang,Jijun Yang,Jiali Liao,Ning Liu
As an excellent target for cancer theranostics, fibroblast activation protein (FAP) has become an attractive focus in cancer research. A class of FAP inhibitors (FAPIs) with a N-(4-quinolinoyl)-Gly-(2-cyanopyrrolidine) scaffold were developed, which displayed nanomolar affinity and high selectivity. Compared with 90Y, 177Lu, 225Ac, and 188Re, 211At seems to be more favored as a therapeutic candidate for FAPI tracers which have fast washout and short retention in tumor sites. Thus, the current study reported the synthesis of two FAPI precursors for 211At and 131I labeling and the preliminary evaluation of 131I-labeled FAPI analogues for cancer theranostics. FAPI variants with stannyl precursors were successfully synthesized and labeled with 131I using a radioiododestannylation reaction. Two radioactive tracers were obtained with high radiochemical purity over 99% and good radiochemical yields of 58.2 ± 1.78 and 59.5 ± 4.44% for 131I-FAPI-02 and 131I-FAPI-04, respectively. Both tracers showed high specific binding to U87MG cells in comparison with little binding to MCF-7 cells. Compared to 131I-FAPI-02, 131I-FAPI-04 exhibited higher affinity, more intracellular uptake, and longer retention time in vitro. Biodistribution studies revealed that both tracers were mainly excreted through the kidneys as well as the hepatobiliary pathway due to their high lipophilicity. In addition, higher accumulation, longer dwell time, and increased tumor-to-organ ratios were achieved by 131I-FAPI-04, which was clearly demonstrated by SPECT/CT imaging. Furthermore, intratumor injection of 131I-FAPI-04 significantly suppressed the tumor growth in U87MG xenograft mice without significant toxicity observed. The above results implied that FAP-targeted alpha endoradiotherapy (specific to 211At) should be used to treat tumors in the near future, considering the chemical similarity between iodine and astatine can ensure the labeling of the latter onto the designed FAPIs.
研究领域:
肿瘤学
·
核医学
·
分子影像学
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DOI
PubMed
高影响因子
ACS Applied Bio Materials
·
2018
·
IF 0
Caixia Sun,Yifan Xu,Lijuan Deng,Hao Zhang,Qiao Sun,Chongjun Zhao,Zhen Li
Black phosphorus (BP) nanostructures have been receiving enormous attention in diverse bioapplications owing to their unique physicochemical properties. However, it is still challenging to investigate their blood circulation, biodistribution, and pharmacokinetics after administration due to the difficulty in quantifying them. Here, we report the quantification of blood circulation, biodistribution, and pharmacokinetics of dextran-modified BP nanoparticles (i.e., BP-DEX NPs) in balb/c mice through the highly sensitive noninvasive photoacoustic (PA) imaging and single-emission computed tomography/computed tomography (SPECT/CT) imaging. We first prepare water-soluble and biocompatible small BP-DEX NPs and label them with radioisotopes 99mTc. We then quantify their half-lives of distribution and elimination phases to be 0.2 and 9.5 h by counting the γ-emissions in the blood of mice administrated with BP-DEX NPs. We also show the dynamic variation of BP-DEX NPs in the tumor, liver, spleen, and kidney through in vivo PA imaging and illustrate the accumulation of nanoparticles in major organs by SPECT/CT imaging, which follows an order of spleen > liver > lung > kidney. Our work demonstrates the renal clearance and hepatobiliary excretion of BP-DEX NPs, which could be potentially translated for clinical in vivo imaging and therapy of cancer.
研究领域:
生物医学工程
·
纳米医学
·
药物递送
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产品关联
DOI
PubMed
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2018
·Vol. 316
·期 2
·685-690
·
IF 1.181
Song Hu,Wang Yunhan,Wang Jing,Wang Guanquan,He Jiaheng,Wei Hongyuan,Luo Shunzhong
For the superiority of graphene quantum dots (GQDs) in bioimaging and drug delivery carrier, GQDs bring new opportunities for theranostics of diseases. In this study, GQDs were successfully prepared and labeled with 131 I. The in vitro properties, biodistribution and SPECT imaging of 131 I-GQDs were investigated. The uptake of 131 I-GQDs at tumor sites can be clearly observed via SPECT imaging and T/B and T/M ratios increase with increasing time, which can contribute to enhanced permeability and retention (EPR) effect.
研究领域:
核医学
·
放射学
·
材料科学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
BIOCONJUGATE CHEMISTRY
·
2016
·
IF 4.5
Jianbo Li,Dawei Jiang,Baoliang Bao,Yulin He,Lei Liu,Xuemei Wang
Self-assembled DNA nanostructures, as a new type of nanocarriers, have shown great potential in molecular imaging probes. DNA bipyramid nanostructures (DBNs), as a classic kind of DNA nanostructure, can be precisely constructed through the unparalleled base-pairing precision of oligonucleotide strands. DBNs were prepared by self-assembly of six oligonucleotides with equal molar amounts in a single annealing step, and purified by high performance liquid chromatography (HPLC). DBNs were stable in 10% FBS as well as 80% mouse serum for at least 8 h. To prepare 99mTc-labeled DBNs, N-hydroxysuccinimidyl S-acetylmercaptoacetyl triglycinate (Sacetyl-MAG3-NHS ester) tagged single-stranded DNA (ssDNA) was first radiolabeled with Tc-99m, and DBNs with an overhang were assembled and then hybridized with 99mTc-ssDNA to prepare 99mTc-labeled DNA bipyramid nanostructures (99mTc-MAG3-DBNs). DBNs were radiolabeled, with the radiochemical purity being over 90%. The plasma half-life of 99mTc-MAG3-DBNs in normal KM mice was about 6 min. The biodistribution and SPECT/CT imaging were conducted with 99mTc-MAG3-DBNs in KM mice, and both showed that 99mTc-MAG3-DBNs mainly concentrated in the intestine, liver, and kidneys, and there was also prominent uptake in the gallbladder and bladder. We successfully obtained a new class of SPECT molecular probes based on this DNA polyhedron structure.
研究领域:
核医学
·
分子影像
·
生物化学
·
放射学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2023
·Vol. 332
·期 6
·2093-2102
·
IF 1.6
Li Kehong,Fan Wenqi,Yan Jingxuan,Wang Jing,Zhao Peng,Liao Wei,Yang Yuchuan,Yang Xia,Wei Hongyuan,Chen Yue
Differences in cellular radiosensitivity and the binding affinity of radiopharmaceuticals could directly affect the radiotherapeutic effects. In this study, we investigated the radionuclide ( 177 Lu) induced radiosensitivity of serval non-small-cell lung cancer cells (NSCLCs) as well as the binding affinity of cetuximab to those cells. The apoptosis of NSCLCs caused by 177 Lu was related to the DNA double-strand damage and was cell-type dependent. We also proved that the introduction of 177 Lu to the antibody could enhance its cytotoxic effect on NSCLCs. The [ 177 Lu]Lu-DOTA-cetuximab could accumulate in the HCC827 tumor xenografts with excellent stability according to in vivo SPECT/CT imaging and the biodistribution results. The [ 177 Lu]Lu-DOTA-cetuximab showed high potential to be used for targeting diagnosis and radiotherapy in lung cancers.
研究领域:
肿瘤学
·
放射生物学
·
核医学
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产品关联
DOI
高影响因子
BIOMATERIALS
·
2020
·
IF 10.317
Xue Zhou,Ning Yan,Erik J. Cornel,Haidong Cai,Shaobo Xue,Hao Xi,Zhen Fan,Shisheng He,Jianzhong Du
We present a bone-targeting polymer vesicle with excellent single photon emission computed tomography/computed tomography (SPECT/CT) imaging capability and high antitumor drug delivery efficiency as an integrated platform for the simultaneous diagnosing and treatment of malignant bone tumors. This polymer vesicle can be self-assembled from poly( ε -caprolactone) 67 - b -poly[( L -glutamic acid) 6 - stat -( L -glutamic acid-alendronic acid) 16 ] (PCL 67 - b -P[Glu 6 - stat -(Glu-ADA) 16 ]), directly in water without the aid of a cosolvent . SPECT/CT dynamically tracked the drug distribution in the bone tumor rabbit models, and the tumor size was significantly reduced from >2.0 cm 3 to <0.6 cm 3 over 11 days. The pathological analysis demonstrated obvious necrosis and apoptosis of the tumor cells. Overall, this bone-targeting polymer vesicle provides us with a new platform for the combination of real-time diagnosis and therapy of malignant bone tumors.
研究领域:
药学
·
生物医学工程
·
癌症研究
·
纳米技术
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ORGANIC CHEMISTRY
·
2019
·
IF 4.745
Ling Yin,Hao Sun,Meng Zhao,Anna Wang,Shanshan Qiu,Yinjia Gao,Jianan Ding,Shun-Jun Ji,Haibin Shi,Mingyuan Gao
Lymphatic metastasis is an important prognostic indicator for cancer progression. It is therefore considerably meaningful to develop molecularly targeted imaging probes for noninvasive and accurate identification of metastatic lymph nodes (MLNs) at early stages of tumor metastasis. Herein, we report a novel matrix metalloproteinase-2 (MMP-2)-activatable probe constructed with a near-infrared dye (Cy5), a quencher (QSY21), and a tumor-targeting peptide cRGD covalently linked through a radionuclide (125I)-labeled peptide substrate for accurate detection of MLNs. Upon cleavage with activated MMP-2, the above probe emitted MMP-2 concentration-dependent near-infrared fluorescence, which allows sensitive and specific visualization of MLNs via both optical and single-photon emission computed tomography imaging techniques. We thus envision that this probe would serve as a useful tool for studying tumor-induced lymphangiogenesis.
研究领域:
癌症生物学
·
分子影像学
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
MATERIALS & DESIGN
·
2022
·
IF 9.417
Yibin Yu,Chong Huang,Fen Chen,Weisan Pan,Ling Zhang
Integration of diagnostic and therapeutic modalities into a single nanoplatform can play an important role in personalized cancer therapy. In this work, an all-in-one theranostic nanoplatform (HPCT nanomicelles) for breast cancer was fabricated, composed of the synthetic polymer hyaluronan- b -poly(ε-caprolactone) (HA-PCL), drug curcumin (Cur) and adjuvant tocopheryl polyethylene glycol succinate (TPGS). HPCT nanomicelles presented adequate drug loading efficiency, excellent stability, and attractive hyaluronidase-sensitive release features. Imaging agent radionuclide 99m Tc was loaded into HPCT nanomicelles (denoted as 99m Tc-HPCT nanomicelles) and in vivo SPECT/CT imaging verified the HA-based nanomicelles could actively target breast cancer in mice. In vivo anti-tumor pharmacodynamic studies indicated that HPCT nanomicelles exhibited desirable anti-tumor efficacy with favorable biosafety. 99m Tc-HPCT nanomicelles, integrating imaging and therapeutic modalities, have the promising potential to be an all-in-one theranostic nanoplatform for breast cancer.
研究领域:
癌症治疗
·
纳米技术
·
药学
·
诊断成像
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）