P2X受体调节剂的作用机制与最新研究进展

Mechanism and recent advances of P2X receptor modulators

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。

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.