中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
  4. 新药研究国家重点实验室
Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic Potential

文献类型：期刊论文

作者Zhang, Yu6; Tan, Ye6; Zhang, Zian2,5; Cheng, Xi1,3; Duan, Jia4,6; Li, Yi2,5,6
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2024-09-13
卷号67期号:18页码:16018-16034
ISSN号0022-2623
DOI10.1021/acs.jmedchem.4c01525
通讯作者Cheng, Xi(xicheng@simm.ac.cn) ; Duan, Jia(duanjia@simm.ac.cn) ; Li, Yi(liyi@simm.ac.cn)
英文摘要TSHR is a member of the glycoprotein hormone receptors, a subfamily of class A G-protein-coupled receptors and plays pivotal roles in various physiological and pathological processes, particularly in thyroid growth and hormone production. The aberrant TSHR function has been implicated in several human diseases including Graves' disease and orbitopathy, nonautoimmune hyperthyroidism, hypothyroidism, cancer, neurological disorders, and osteoporosis. Consequently, TSHR is recognized as an attractive therapeutic target, and targeting TSHR with small-molecule modulators including agonists, antagonists, and inverse agonists offers great potential for drug discovery. In this perspective, we summarize the structures and biological functions of TSHR as well as the recent advances in the development of small-molecule TSHR modulators, highlighting their chemotypes, mode of actions, structure-activity relationships, characterizations, in vitro/in vivo activities, and therapeutic potential. The challenges, new opportunities, and future directions in this area are also discussed.
WOS关键词HUMAN THYROTROPIN RECEPTOR ; ENDOTHELIAL GROWTH-FACTOR ; TSH RECEPTOR ; GRAVES-DISEASE ; INVERSE AGONIST ; CRYSTAL-STRUCTURE ; GENE-EXPRESSION ; ORBITAL TISSUE ; ADIPOSE-TISSUE ; CYCLIC-AMP
资助项目Shanghai Pujiang Program[23PJ1415200] ; National Natural Science Foundation of China[82373881] ; National Natural Science Foundation of China[22101054] ; Young Elite Scientists Sponsorship Program by CAST[2022QNRC001] ; Shanghai Sailing Program[23YF1456800] ; Youth Innovation Promotion Association of Chinese Academy of Sciences[2022077]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001313796100001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/313320]  
专题新药研究国家重点实验室
通讯作者Cheng, Xi; Duan, Jia; Li, Yi
作者单位1.Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 330106, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Struct & Funct Drug Targets, Shanghai 201203, Peoples R China
5.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China
6.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan 528400, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Yu,Tan, Ye,Zhang, Zian,et al. Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic Potential[J]. JOURNAL OF MEDICINAL CHEMISTRY,2024,67(18):16018-16034.
APA Zhang, Yu,Tan, Ye,Zhang, Zian,Cheng, Xi,Duan, Jia,&Li, Yi.(2024).Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic Potential.JOURNAL OF MEDICINAL CHEMISTRY,67(18),16018-16034.
MLA Zhang, Yu,et al."Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic Potential".JOURNAL OF MEDICINAL CHEMISTRY 67.18(2024):16018-16034.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。