《生命科学》 2022, 34(2): 137-144

P2X受体内源性异源三聚体的研究进展

沈晨晖¹ , 陈　曦² , 曹征宇^1,* , 杨晓娜^2,*

¹中国药科大学中药学院，南京 210009 ²中国药科大学基础医学与临床药学学院，南京 210009

摘　要：

离子通道型嘌呤能受体P2X 是一类可被胞外ATP 激活的配体门控阳离子通道，以同源或异源三聚体的形式行使功能。它们广泛分布于全身各组织，参与多种生理病理学过程，是一类重要的新药靶标。由于P2X 异聚体的研究较同聚体复杂，一定程度上阻碍了其特异性靶向药物的研发。本文就P2X 异聚体的成员分类、亚基组成计量学、参与的生理病理过程以及相关靶向药物研发进行了综述。

通讯作者：曹征宇 , Email:zycao1999@hotmail.com 杨晓娜 , Email:yangxiaona@cpu.edu.cn

Advances in the study of endogenous heterotrimers of P2X receptors

SHEN Chen-Hui¹ , CHEN Xi² , CAO Zheng-Yu^1,* , YANG Xiao-Na^2,*

¹School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China ²School of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing 210009, China

Abstract:

Purinergic P2X receptors, a class of ligand-gated cation channels, can be activated by extracellular ATP and function as homo- or heteromeric trimers. They are widely distributed in various tissues of the body and involved in various physiological and pathological processes, making them an important target for new drugs. The study of P2X heterotrimers is more complex than homotrimers, which to some extent hinders the development of specific targeted drugs. Herein, we review the various heteromeric assemblies of P2X subtypes, the stoichiometry and physiological and pathological functions of the heteromeric P2X receptors, and the related P2X targeted drug development.

Communication Author：CAO Zheng-Yu , Email:zycao1999@hotmail.com YANG Xiao-Na , Email:yangxiaona@cpu.edu.cn