Structural Pharmacology of TRP Channels. Issue 17 (20th August 2021)

• Record Type: Journal Article
• Authors: Zhao, Yaxian; McVeigh, Bridget M.; Moiseenkova-Bell, Vera Y.
• Is Part Of: Journal of molecular biology. Volume 433:Issue 17(2021)
• Publication Date: 2021-08-20
• Subjects: ion channels -- TRP channel -- structural biology -- cryo-EM; Molecular biology -- Periodicals; Biology -- Periodicals; Biochemistry -- Periodicals; Bacteriology -- Periodicals; Molecular Biology -- Periodicals; Biochemistry -- Periodicals; Biologie moléculaire -- Périodiques; Biologie -- Périodiques; Biochimie -- Périodiques; Moleculaire biologie; Biochemistry; Biology; Molecular biology; Periodicals; 572.805
• DOI: 10.1016/j.jmb.2021.166914
• Languages: English
• ISSNs: 0022-2836

Abstract

Graphical abstract: Highlights: TRP channel subfamilies have distinguishing structural features. Conserved binding pockets across TRP channels. The S4-S5 linker and TRP helix serve as a signaling platform. Abstract: 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.