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Structural Pharmacology of TRP Channels.


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.

SUBMITTER: Zhao Y 

PROVIDER: S-EPMC8338738 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature

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Structural Pharmacology of TRP Channels.

Zhao Yaxian Y   McVeigh Bridget M BM   Moiseenkova-Bell Vera Y VY  

Journal of molecular biology 20210305 17


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  ...[more]

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