The capsaicin binding affinity of wildtype and mutant TRPV1 ion channels.

ABSTRACT: Vanilloids such as capsaicin and resiniferatoxin are highly selective and potent activators for transient receptor potential vanilloid subfamily, member 1, a nociceptor for heat and pain perception. However, the intrinsic vanilloid binding affinity, key for understanding transient receptor potential vanilloid subfamily, member 1 function, remains unknown despite intensive investigations by electrophysiological, structural, and computational methods. In this study, we determined capsaicin binding affinity under physiological conditions by isolating individual binding steps to each subunit with concatemers. We estimated the capsaicin association constant of a wildtype subunit to be in the order of 10⁶ M^-1 and that of the Y511A mutant subunit to be a hundred times lower,

SUBMITTER: Li S 

PROVIDER: S-EPMC10616419 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature