MOLECULAR PHARMACEUTICS
·
2024
·
IF 4.5
Zuojie Li,Yuhao Jiang,Qing Ruan,Guangxing Yin,Peiwen Han,Xiaojiang Duan,Junbo Zhang
The specific expression of prostate-specific membrane antigen (PSMA) makes it an ideal target for the diagnosis and treatment of prostate cancer. Currently, many 99mTc-labeled PSMA-targeted tracers have been developed. However, the high renal uptake of these 99mTc-labeled tracers is a common problem that limits their clinical application. In this work, the ligand (EUKPG) using DPro-Gly as the linker was synthesized and three 99mTc-labeled complexes ([99mTc]Tc-EUKPG-EDDA, [99mTc]Tc-EUKPG-TPPTS, [99mTc]Tc-EUKPG-TPPMS) with different coligands were prepared and evaluated. Among them, [99mTc]Tc-EUKPG-EDDA showed the most favorable pharmacokinetic properties, with significantly reduced uptake in the kidney (14.04 ± 0.23% ID/g), rapid clearance and low uptake in nontarget organs, thus making it to exhibit high tumor-to-background ratios (tumor/blood: 7.47, tumor/muscle: 12.65). Affinity studies have shown that it has high specificity for PSMA both in vivo and in vitro. Therefore, [99mTc]Tc-EUKPG-EDDA has great potential as a promising molecular tracer to target PSMA for tumor imaging.
研究领域:
医学影像学
·
肿瘤学
·
放射化学
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DOI
PubMed
高影响因子
ACS Sensors
·
2025
·
IF 9.1
Zuhua Zeng,Ying Tan,Tiantian Luo,Zhengwei Li,Guihao Hu,Yao Liu,Ling He,Haiyu Wang,Lei Zhong,Haiying Wang,Tianwei Liu,Jiang Zhu
Melanoma is one of the most aggressive forms of skin cancer. Accurate and early diagnosis of melanoma is crucial for improving patient outcomes. This study develops two TYR-activatable molecular probes, Mn-TyrEDTA and Al-18F-TyrEDTA, for the selective detection of melanoma in vivo. In vitro studies reveal that Mn-TyrEDTA exhibits TYR activity-dependent relaxivity enhancement, undergoing TYR-mediated oxidative polymerization, resulting in the formation of paramagnetic oligomers. UV–vis analysis supports this mechanism, showing time- and TYR concentration-dependent increases in broad band absorbance in the UV–vis region, specifically around 475 nm, due to the formation of o-quinone intermediates and melanin-like oligomers. HPLC analysis further confirmed the presence of polar oligomeric products in Mn-TyrEDTA solutions incubated with TYR/O2. MRI studies demonstrate Mn-TyrEDTA’s selective retention and signal enhancement in TYR-expressing melanoma tissues. Furthermore, PET imaging with Al-18F-TyrEDTA conducted using a dual-xenograft mouse model reveals significantly higher uptake and retention of Al-18F-TyrEDTA in TYR-expressing melanoma compared to TYR-negative tumors. This selective retention could be attributed to a TYR-mediated proximity labeling mechanism, where highly reactive quinones form covalent bonds with nearby tumor proteins. In summary, our findings establish Mn-TyrEDTA and Al-18F-TyrEDTA as promising TYR-activatable imaging probes, offering a novel strategy for the early diagnosis and prognosis of melanoma.
研究领域:
医学影像学
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肿瘤学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
Journal of Materials Chemistry B
·
2016
·Vol. 4
·期 23
·4110-4118
·
IF 4.872
Jing Zhang,Guangyu Hao,Chenfei Yao,Su Hu,Chunhong Hu,Bingbo Zhang
Glioma stem cells (GSCs) are considered the key to the occurrence, development, invasion, recurrence and sensitivity to treatment of brain tumors. Precise molecular imaging of GSCs by means of probes in vivo has therefore become a premise of solving the above problems. Herein, a sensitive, specific, accurate and biocompatible molecular nanoprobe is reported with MR/fluorescence imaging modalities for CD133+ glioma tumor bimodal targeted imaging. Cd-free high quality CuInS2/ZnS core/shell quantum dots (QDs) were synthesized for fluorescence imaging; DTPA-coupled BSA with Gd3+ chelation (BSA-DTPAGd) were prepared and used both for phase transfer of hydrophobic CuInS2/ZnS QDs and MR imaging modality. The resulting hydrophilic paramagnetic QDs (pQDs) were then linked with anti-CD133 monoclonal antibody, pQDs-CD133mAb denoting the framework of the entire molecular probe, for tumor targeting. The obtained pQDs-CD133mAb has a proper size (ca. 45 nm) and good colloidal stability. It exhibits a high quality fluorescent emission (ca. 630 nm) together with high longitudinal relaxivity (r1 = 15.2 mM−1 s−1) compared with that of commercial Magnevist (r1 = 3.12 mM−1 s−1). Dual modal imaging in vitro and in vivo shows potent tumor enhancement with administration of pQDs-CD133mAb. A biodistribution study indicates hepatobiliary and renal processing of pQDs-CD133mAb with no obvious toxicity. It could be therefore concluded, with a dual-modal imaging and targeting strategy, pQDs-CD133mAb presents a great potential as an alternative for accurate diagnosis of glioma.
研究领域:
医学影像学
·
肿瘤学
·
纳米医学
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产品关联
DOI
PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2020
·
IF 3.232
Wenjun Zhou,Qiang Gao,Darui Liu,Chen Li,Shu Liu,Kaisheng Xia,Bo Han,Chenggang Zhou
A novel salicylaldehyde bis-Schiff-base probe decorated with imidazolium ionic liquid moieties at both ends (SAS-IMIs) was designed and facilely synthesized as a colorimetric/ratiometric sensor to visually detect Cu 2+ and Pd 2+ in pure aqueous media. Due to the positively charged characters of its head and tail, the SAS-IMIs exhibited high water solubility with a potential advantage in minimizing the self-aggregation. More importantly, simply by varying the solution pH, colorimetric/ratiometric sensing detection of individual metal ion (Cu 2+ or Pd 2+ ) was realized without any mutual interference. Subsequently, sensitive, selective, and differential detections for Cu 2+ (LOD: 0.080 μM) and Pd 2+ (LOD: 0.076 μM) in 100% aqueous solutions were achieved, which proved to be applicable for real water samples. Results from density functional theory (DFT) calculations unveiled the Cu 2+ /Pd 2+ -binding properties of SAS-IMIs, which were in accordance with the experimental observations. Furthermore, a SAS-IMIs-based solid phase sensor was fabricated, which manifested satisfactory detection abilities for Cu 2+ and Pd 2+ .
研究领域:
分析化学
·
环境科学
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产品关联
DOI
PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2023
·
IF 4.4
Brian Musikavanhu,Zeping Huang,Quanhong Ma,Yongdi Liang,Zhaoli Xue,Lei Feng,Long Zhao
A pyridine modified naphthol hydrazone Schiff base chemosensor, NaPy , was prepared in a two-step process to detect aluminum ion (Al 3+ ) in different samples. The probe shows a turn-off emission response towards Al 3+ at a 1:1 binding stoichiometry via intramolecular charge transfer (ICT) mechanism, as validated by density functional theory (DFT) calculations and a series of spectroscopic measurements. The response time is slightly over one minute with a limit of detection (LOD) value of 0.164 µM, demonstrating the great sensitivity of the probe. It is also found that NaPy exhibits high selectivity towards Al 3+ and resists interference from seventeen other cations. Application investigations in paper strips, water samples and HeLa cells suggest that NaPy can be used as an efficient probe for sensing Al 3+ in real environmental samples and biosystems.
研究领域:
分析化学
·
环境科学
·
生物医学
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产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2023
·
IF 9.5
Lei Xia,Chengxue He,Yanhui Guo,Xiangxi Meng,Teli Liu,Xiaoxia Xu,Xiaoyi Guo,Feng Wang,Nan Li,Hua Zhu,Zhi Yang
Programmed death ligand 1 (PDL1) is a specific molecular target for the diagnosis and immunotherapy of solid tumors. PET imaging can be used for noninvasive assessments of PDL1 expression in tumors to aid in therapy selection. The most frequently reported small-molecule radiotracer of PDL1 is limited by low imaging specificity, short residence time, and singular functionality. Here, we combined a biocompatible melanin nanoprobe with the PDL1-binding peptide WL12 to construct a novel radiotracer, 124I-WPMN, to enhance PDL1 targeting. The radiochemical purity of 124I-WPMN was >95%, and uptake in A549PDL1 cells was 1.49 ± 0.08% at 2 h. The uptake was blocked by WL12 (0.39 ± 0.03%, P < 0.0001). This novel radiotracer showed a higher affinity for PDL1 (Kd = 18.5 nM) than 68Ga-NOTA-WL12 (Kd = 24.0 nM). Micro-PET/CT imaging demonstrated specific uptake and a high signal-to-noise ratio in an A549PDL1 xenograft mouse model with a tumor-to-muscle ratio of 27.31 ± 7.03 at 2 h. The levels increased or remained steady for more than 72 h, and tumor uptake was significantly higher than 68Ga-NOTA-WL12, at 6.08 ± 0.62 at 2 h. Prolonged retention of 124I-WPMN makes it possible to conduct PET/MRI imaging over long periods and to perform various imaging techniques. A clear advantage of 124I-WPMN over 68Ga-NOTA-WL12 was observed for PDL1-targeted PET imaging after nanoparticle modification, supporting the utility of 124I-WPMN PET imaging as an effective diagnostic tool for optimizing PDL1-targeted therapies.
研究领域:
肿瘤学
·
医学影像
·
生物化学
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DOI
PubMed
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
·
2017
·
IF 5.401
Ce-Ce Hu,Qiang Gao,Li-Li Chang,Dan Luo,Bo Han,Kai-Sheng Xia,Cheng-Gang Zhou
Expanding the availability of hydrophobic small-molecule probes in pure aqueous environments is an important issue likely to significantly impact their application prospects in sensing detections. The present work demonstrates for the first time that poly(ionic liquid) (PIL) can serve as a superior carrier, which not only enables hydrophobic small-molecule probes to readily disperse in pure water and but helps maximize their sensing performances. As a proof-of-concept, a hydrophobic rhodamine derivative carried by PIL, P(RhBHSA-co-META), was designed and applied for the colorimetric determination of Cu 2+ and further for CN − in fully aqueous solutions. Due to the positively charged nature of polymeric backbone, the P(RhBHSA-co-META) was highly water-soluble and could avoid non-specific bonding. Moreover, the strong inter- and intra-chain electrostatic repulsions made the P(RhBHSA-co-META) possible to be fully free and highly stretched in water, facilitating the accessibility of receptor binding sites. Excellent sensing performance of P(RhBHSA-co-META) toward Cu 2+ was achieved in terms of high sensitivity, ultrafast color/absorption response, and excellent anti-disturbance ability. Furthermore, the pre-formed P(RhBHSA-co-META)–Cu 2+ complex was also verified to be highly efficient for colorimetric determination of CN − , exhibiting high sensitivity and selectivity. This study provides a simple, effective, and extendable approach for designing water-soluble chemosensors for ion detections and other sensing applications.
研究领域:
分析化学
·
材料科学
·
环境科学
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DOI
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2018
·Vol. 42
·期 17
·14325-14331
·
IF 3.201
Ruiqing Feng,Longlong Li,Bing Li,Jinhui Li,Dan Peng,Yitao Yu,Qiuhong Mu,Ning Zhao,Xiaoqiang Yu,Zhenhua Wang
We have synthesized a two-photon organic small-molecule probe (DMI), which has a considerable two-photon absorption cross section (δ) value and selectively stained endogenous RNA in the nucleolus and the cytoplasm of living cells with outstanding membrane permeability. The titrations, fluorescence imaging and RNase digest test indicate markedly higher affinity for endogenous RNA. The double assay of DMI and SYTOX Blue nucleic acid stain (S-11348) showed that the probe possesses excellent membrane permeability to living cells, and a co-staining experiment with the classic DNA-staining dye DAPI indicated that it has excellent counterstain compatibility. Moreover, DMI exhibited good photostability when continuously illuminated by constant femtosecond pulses. These results demonstrate that DMI is an attractive two-photon fluorescent probe for visualizing RNA in living cells.
研究领域:
生物化学
·
细胞生物学
·
分子影像学
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产品关联
DOI
高影响因子
ANALYTICA CHIMICA ACTA
·
2023
·
IF 6.2
Zhongyong Xu,Chao Song,Zihao Chen,Conghui Zeng,Taoyuze Lv,Lei Wang,Bin Liu
Nitroxynil (NTX) is a common anthelmintic veterinary drug for the management of fascioliasis in food-producing sheep and cattle. Since excessive NTX residue in food can lead to several adverse side effects, such as allergic skin reaction and respiratory irritation, it is of great importance to develop an efficient analytical method for NTX determination. Herein, we report a simple fluorescent detection method based on a novel supramolecular probe capable of detecting NTX with a fast response (5 s), high sensitivity (107 nM), high selectivity , and acceptable anti-interference property. Moreover, the portable paper-based test strips were facilely prepared and successfully realized on-site determination of NTX in real edible animal products simply with the aid of a smartphone. To the best of our knowledge, this is the very first report on the portable detection of NTX. This study also provides a promising strategy for the fast and portable detection of analyte based on the host-guest system, which will lead to improved fluorescent probe design for food analysis.
研究领域:
食品安全
·
分析化学
·
兽医学
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DOI
PubMed
高影响因子
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
✓ 已验证
DOI
高影响因子
INORGANIC CHEMISTRY
·
2018
·
IF 4.7
Xiangqian Li,Zhan Zhou,Cheng Cheng Zhang,Yuhui Zheng,Jinwei Gao,Qianming Wang
A novel optical nanoprobe based on silicon quantum dots (SiQDs) has been assembled through a one-pot low-temperature (40 °C) treatment by using 3-(aminopropyl)trimethoxysilane (APTMS) and ascorbic acid (AA) as two precursors. The water-soluble SiQDs demonstrate intense green luminescence in aqueous environment and the excitation-dependent feature has been explored. Meanwhile, the incorporation of salicylaldehyde (SA) serves to suppress the emission of SiQDs effectively via nucleophilic reaction and an “on–off” change is observed. Furthermore, the addition of Zn2+ can lead to evolution of emission peaks, and the green band at 500 nm gradually shifts toward the blue side at 455 nm. The corresponding ratiometric signal changes (I455/I500) can accurately determine the Zn2+ concentration and the limit of detection is calculated to be 0.17 μM in the linear range between 1 and 100 μM. In this research, a molecular logic gate (AND) system has been well established by using SA and Zn2+ as two inputs. The fluorescence emission changes based on SiQDs will shed new light on the development of functional sensors at the nanoscale level.
研究领域:
纳米材料科学
·
分析化学
·
生物传感
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Analytical Methods
·
2025
·
IF 2.6
Changqing Du,Anran Li,Jinye Qiu,Jiarui Sun,Xiaokun Wang,Wei Xu,Maofeng Zhang,Dapeng Wang
Quantitative mRNA expression levels are essential for differential and clinical diagnoses. In this work, we present an apurinic/apyrimidinic endonuclease 1 (APE1)-assisted SERS sensing platform for rapid and ultrasensitive detection of TK1 mRNA. This platform utilizes a hairpin probe that contains a TK1 mRNA capture sequence along with an apurinic/apyrimidinic (AP) sites, which is specifically recognized and cleaved by APE1. Upon introduction of the target mRNA, hybridization occurs between the mRNA and the AP probe (HAP) within the hairpin structure, forming a doublestranded complex. APE1 then cleaves the HAP at the specific AP sites within the double-stranded complex, leading to a measurable change in the SERS intensity of the FAM-labeled HAP. Based on this principle, the developed SERS sensing platform demonstrates a highly linear response for TK1 mRNA detection across a wider range from 1 fM to 10 nM, with a detection limit (LOD) of 0.2 fM. Moreover, the SERS sensing platform shows great potential for the precise and quantitative detection of TK1 mRNA in human serum, which could be instrumental for mRNA-related research and the early clinical diagnosis of diseases.
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产品关联
DOI
PubMed
高影响因子
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