Structural Pharmacology of TRP Channels

Transient receptor potential (TRP) ion channels are a super-family of ion channels that mediate transmembrane cation flux with polymodal activation, ranging from chemical to physical stimuli. Furthermore, due to their ubiquitous expression and role in human diseases, they serve as potential pharmacological targets. Advances in cryo-EM TRP channel structural biology has revealed general, as well as diverse, architectural elements and regulatory sites among TRP channel subfamilies. Here, we review the endogenous and pharmacological ligand-binding sites of TRP channels and their regulatory mechanisms. (C) 2021 Elsevier Ltd. All rights reserved.

Automated summary

TRP ion channels are a super-family that mediate transmembrane cation flux in response to various stimuli. Recognized as potential pharmacological targets due to their role in human diseases, advances in cryo-EM TRP channel structural biology have shown diverse architectural elements and regulatory sites. This review focuses on the ligand-binding sites and regulatory mechanisms of TRP channels.