TRPV6 Regulation by Cis-22a and Cholesterol.

ABSTRACT: The highly calcium-selective transient receptor potential vanilloid-type channel TRPV6 is important for epithelial Ca²⁺ transport. Proper regulation of the inherently constitutively active TRPV6 channels is intricate in preserving Ca²⁺ homeostasis, whereby structural and functional data suggest that lipids hold an essential role. Altered expression levels or specific TRPV6 mutations may lead to diseases, hence, TRPV6 represents an interesting target for pharmacological modulation. Recent cryo-EM data identified that the specific TRPV6 blocker cis-22a binds, apart from the pore, to a site within the tetrameric channel that largely matches a lipid binding pocket, LBS-2. Therein, cis-22a may replace a lipid such as cholesterol that is bound in the open state. Based on si

SUBMITTER: Humer C 

PROVIDER: S-EPMC9221249 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature