Radiosynthesis and Biological Evaluation of a Small-Molecule Probe for Thyroid-Stimulating Hormone Receptor
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DOI:
文献链接: https://pubs.acs.org/doi/10.1021/acsmedchemlett.5c00210
其他信息:
Y Zhou, J Tao, Y Jiang, A Ji, X Luo, J Tian…
ACS Medicinal …, 2025
ACS Publications
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 131I-ML-109, and its biological performance was further evaluated as a single-photon emission computed …
