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Radiosynthesis and Biological Evaluation of a Small-Molecule Probe for Thyroid-Stimulating Hormone Receptor

文献类型：期刊论文

作者Zhou, Yuanyuan3,4; Tao, Ji4; Jiang, Yuanpeng4,5; Ji, Aiyan4; Luo, Xiangning4; Tian, Jin3,4; Zhao, Xuanyan4; Qian, Kun4; Qu, Chunrong4; Wang, Renfei1
刊名ACS MEDICINAL CHEMISTRY LETTERS
出版日期2025-09-11
卷号16期号:9页码:1740-1746
关键词Thyroid-stimulating hormone receptor Thyroid cancer Small-molecule TSHR agonist I-131
ISSN号1948-5875
DOI10.1021/acsmedchemlett.5c00210
英文摘要The thyroid-stimulating hormone receptor (TSHR) plays a pivotal role in regulating thyroid growth, function, synthesis, and secretion of thyroid hormones, with its overexpression linked to various diseases, especially in tumors. A novel TSHR-targeting small molecule agonist ML-109 with a nM potency has been developed. In this study, we radiolabeled ML-109 with radionuclide iodine-131 on the quinazolin-4-one ring to prepare I-131-ML-109, and its biological performance was further evaluated as a single-photon emission computed tomography radiotracer. The results displayed that I-131-ML-109 was prepared in high radiochemical purity >95% and moderate radiolabeling yield (similar to 40%). Further, I-131-ML-109 demonstrated a good tumor uptake capability in both K1 and 8305C xenograft models. Overall, this study has established the synthetic strategy for preparation of I-131-ML-109, highlighting that ML-109 is a promising molecular scaffold for developing TSHR targeted imaging probe. Further structural optimization is desired to improve the diagnostic performance of the next-generation probe.
WOS关键词THYROTROPIN RECEPTOR ; TSH RECEPTOR ; AGONISTS ; EXPRESSION ; CANCER
资助项目National Natural Science Foundation of China[U2267221] ; State Key Laboratory of Drug Research[SIMM0120231004] ; Ningbo Major Research and Development Plan Project[2024Z214] ; Natural Science Foundation of Shanghai[24ZR1477300] ; Shandong Laboratory Program[SYS202205]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001547521600001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/321258]  
专题国家级研究中心_原创新药研究全国重点实验室
通讯作者Wang, Renfei; Chen, Wen-Hua; Cheng, Zhen
作者单位1.Tongji Univ, Shanghai Peoples Hosp 10, Sch Med, Dept Nucl Med, Shanghai 200072, Peoples R China
2.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China
3.Wuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Guangdong, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Mol Imaging Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China
5.Univ Chinese Acad Sci, Sch Pharm, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Zhou, Yuanyuan,Tao, Ji,Jiang, Yuanpeng,et al. Radiosynthesis and Biological Evaluation of a Small-Molecule Probe for Thyroid-Stimulating Hormone Receptor[J]. ACS MEDICINAL CHEMISTRY LETTERS,2025,16(9):1740-1746.
APA Zhou, Yuanyuan.,Tao, Ji.,Jiang, Yuanpeng.,Ji, Aiyan.,Luo, Xiangning.,...&Cheng, Zhen.(2025).Radiosynthesis and Biological Evaluation of a Small-Molecule Probe for Thyroid-Stimulating Hormone Receptor.ACS MEDICINAL CHEMISTRY LETTERS,16(9),1740-1746.
MLA Zhou, Yuanyuan,et al."Radiosynthesis and Biological Evaluation of a Small-Molecule Probe for Thyroid-Stimulating Hormone Receptor".ACS MEDICINAL CHEMISTRY LETTERS 16.9(2025):1740-1746.

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来源：上海药物研究所

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