Photoswitchable TRPC6 channel activators evoke distinct channel kinetics reflecting different gating behaviors.

ABSTRACT: The non-selective transient receptor potential canonical 6 (TRPC6) cation channels have several physiological and pathophysiological effects. They are activated by the lipid second messenger diacylglycerol (DAG) and by non-lipidic compounds such as GSK 1702934A (GSK). Advances in photopharmacology led to the development of photoswitchable activators such as PhoDAG, OptoDArG, and OptoBI-1 that can be switched ON and OFF with the spatiotemporal precision of light. We aimed to elucidate whether these photopharmaceuticals allow for a reliable determination of the ion channel current kinetics. We performed electrophysiological whole-cell measurements in the overexpression system and analyzed TRPC6 currents induced by photoswitching. We observed distinct activation, deactivation and inact

SUBMITTER: Keck M 

PROVIDER: S-EPMC11472632 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature