张 萌1,2,3 , 卢向阳1 , 田 云1,3,* , 杨晓娜1,*
1湖南农业大学生物科学技术学院,长沙 410128 2湖南绿蔓生物科技股份有限公司,长沙 410013 3湖南甜蔓生物科技有限公司,永州 425900

摘 要:

ATP 激活的配体门控阳离子通道P2X 受体参与多种生理病理功能,是一类重要的新药靶标。目前发现的多种靶向P2X 受体的小分子药物多数因结果未达到预期或存在明显的副作用而止步于临床研究。明确的调节机制可为靶向P2X 受体的理性药物设计提供新的方向,从而提高药物发现概率和有效性。本文就P2X 受体调节剂的作用机制进行综述,并对靶向P2X 受体的小分子药物最新研究进展进行总结。

通讯作者:田 云 , Email:tianyun79616@163.com 杨晓娜 , Email:yangxiaona@hunau.edu.cn

Mechanism and recent advances of P2X receptor modulators
ZHANG Meng1,2,3 , LU Xiang-Yang1 , TIAN Yun1,3,* , YANG Xiao-Na1,*
1College of Bioscience and Biotechnology, Hunan Agricultural University, Changsha 410128, China 2Hunan Nutramax Inc., Changsha 410013, China 3Hunan Sweetmax Inc., Yongzhou 425900, China


The P2X receptor, an ATP-activated ligand-gated cation channel, is involved in a variety of physiological and pathological functions and is an important target for new drugs. At present, clinical researches on small molecule drugs targeting P2X receptor are mostly stopped because of the unexpected results or obvious side effects. Clear regulation mechanisms can provide new perspectives for rational drug design targeting P2X receptors, accelerating drug discovery and effectiveness. Here, we review the regulatory mechanisms of P2X receptor modulators and the latest research progress on small molecule drugs targeting P2X receptors.

Communication Author:TIAN Yun , Email:tianyun79616@163.com YANG Xiao-Na , Email:yangxiaona@hunau.edu.cn

Back to top