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Identification, structure, and agonist design of an androgen membrane receptor 期刊论文

编号：

DDDDD35FB621EACDE4EA22008CC531E7
作者：

Yang, Zhao#^[1,2]Ping, YuQi#^[3]Wang, MingWei#^[1,2,4]Zhang, Chao#^[1,2]Zhou, ShuHua#^[1,2,5]Xi, YueTong#^[1,2]Zhu, KongKai#^[1,2]Ding, Wei^[6];Zhang, QiYue^[1,2];Song, ZhiChen^[5];Zhao, RuJia^[5];He, ZiLu^[1];Wang, MengXin^[3];Qi, Lei^[7];Ullmann, Christian^[8];Ricken, Albert^[7,9];Schoneberg, Torsten^[8];Gan, ZhenJi^[10];Yu, Xiao*^[5]Xiao, Peng*^[1,2,3]Yi, Fan(易凡)*^[11]Liebscher, Ines*^[8]Sun, JinPeng*^[1,2]
语种：

英文
期刊：

CELL ISSN：0092-8674 2025 年 188 卷 6 期 (1589 - 1604) ; MAR 20
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摘要：

Androgens, such as 5oc-dihydrotestosterone (5oc-DHT), regulate numerous functions by binding to nuclear androgen receptors (ARs) and potential unknown membrane receptors. Here, we report that the androgen 5oc-DHT activates membrane receptor GPR133 in muscle cells, thereby increasing intracellular cyclic AMP (cAMP) levels and enhancing muscle strength. Further cryoelectron microscopy (cryo-EM) structural analysis of GPR133-Gs in complex with 5oc-DHT or its derivative methenolone (MET) reveals the structural basis for androgen recognition. Notably, the presence of the "F(F/L)2.64-F3.40-W6.53"and the "F7.4233N/D7.46"motifs, which recognize the hydrophobic steroid core and polar groups, respectively, are common in adhesion GPCRs (aGPCRs), suggesting that many aGPCRs may recognize different steroid hormones. Finally, we exploited in silico screening methods to identify a small molecule, AP503, which activates GPR133 and separates the beneficial muscle-strengthening effects from side effects mediated by AR. Thus, GPR133 represents an androgen membrane receptor that contributes to normal androgen physiology and has important therapeutic potentials.
推荐引用方式
GB/T 7714：

Yang Zhao,Ping Yu-Qi,Wang Ming-Wei, et al. Identification, structure, and agonist design of an androgen membrane receptor [J].CELL,2025,188(6):1589-1604.
APA：

Yang Zhao,Ping Yu-Qi,Wang Ming-Wei,Zhang Chao,&Sun Jin-Peng.(2025).Identification, structure, and agonist design of an androgen membrane receptor .CELL,188(6):1589-1604.
MLA：

Yang Zhao, et al. "Identification, structure, and agonist design of an androgen membrane receptor" .CELL 188,6(2025):1589-1604.
入库时间：

2/26/2025 9:33:25 PM
更新时间：

5/7/2025 9:34:17 AM
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