P2X受体内源性异源三聚体的研究进展

Advances in the study of endogenous heterotrimers of P2X receptors

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。

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.