Structural insights into the orthosteric inhibition of P2X receptors by non-ATP analog antagonists.

ABSTRACT: P2X receptors are extracellular ATP-gated ion channels that form homo- or heterotrimers and consist of seven subtypes. They are expressed in various tissues, including neuronal and nonneuronal cells, and play critical roles in physiological processes such as neurotransmission, inflammation, pain, and cancer. As a result, P2X receptors have attracted considerable interest as drug targets, and various competitive inhibitors have been developed. However, although several P2X receptor structures from different subtypes have been reported, the limited structural information of P2X receptors in complex with competitive antagonists hampers the understanding of orthosteric inhibition, hindering the further design and optimization of those antagonists for drug discovery. We determined the cryogenic

SUBMITTER: Sheng D 

PROVIDER: S-EPMC10997329 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature