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Article

Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.

Journal of medicinal chemistry - 26 May 2022

Li Qiu, Yao Benqiang, Zhao Shiting, Lu Zhou, Zhang Yan, Xiang Qiuping, Wu Xishan, Yu Haonan, Zhang Cheng, Li Junhua, Zhuang Xiaoxi, Wu Donghai, Li Yong, Xu Yong

Abstract excerpt

The design and development of agonists selectively targeting thyroid hormone receptor β (TRβ) and TRβ mutants remain challenging tasks. In this study, we first adopted the strategy of breaking the "His-Phe switch" to solve two problems, simultaneously. A structure-based design approach was successfully utilized to obtain compound 16g, which is a potent TRβ agonist (EC50: 21.0 nM, 85.0% of the maximum efficacy of...

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Identifiers

PMID: 35507418
DOI: 10.1021/acs.jmedchem.2c00144

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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