Function and therapeutic potential of G protein-coupled receptors in epididymis.
Function and therapeutic potential of G protein-coupled receptors in epididymis.
复制标题
附睾中 G 蛋白偶联受体的功能和治疗潜力。
DOI：
10.1111/bph.15252
复制
发表时间：
2020
影响因子：
7.3
通讯作者：
Xu Zhigang
中科院分区：
文献类型：
--
作者：
Zhang Daolai;Wang Yanfei;Lin Hui;Sun Yujing;Wang Mingwei;Jia Yingli;Yu Xiao;Jiang Hui;Xu Wenming;Sun Jin-Peng;Xu Zhigang
近年来，女性和男性的不育率持续上升。目前，仍然缺乏具有明确机制或靶点的男性不育症的有效治疗方法。G蛋白偶联受体（GPCR）是最大的一类药物靶点，但它们的功能和对男性不育治疗发展的影响在很大程度上仍然难以捉摸。然而，最近的研究表明，GPCR超家族的几个成员在维持附睾的离子-水稳态、传出小管的发育、血-附睾屏障的形成和精子的成熟中起着至关重要的作用。对这些GPCR的功能、遗传变异和工作机制的了解，沿着与其特定功能相关的药物和配体，为治疗男性不育症的新发展提供了未来的方向和巨大的武器库。
Infertility rates for both females and males have increased continuously in recent years. Currently, effective treatments for male infertility with defined mechanisms or targets are still lacking. G protein‐coupled receptors (GPCRs) are the largest class of drug targets, but their functions and the implications for the therapeutic development for male infertility largely remain elusive. Nevertheless, recent studies have shown that several members of the GPCR superfamily play crucial roles in the maintenance of ion–water homeostasis of the epididymis, development of the efferent ductules, formation of the blood–epididymal barrier and maturation of sperm. Knowledge of the functions, genetic variations and working mechanisms of such GPCRs, along with the drugs and ligands relevant to their specific functions, provide future directions and a great arsenal for new developments in the treatment of male infertility.