CL-705G: a novel chemical Kir6.2-specific K_ATP channel opener.

ABSTRACT: Background: K_ATP channels have diverse roles, including regulation of insulin secretion and blood flow, and protection against biological stress responses and are excellent therapeutic targets. Different subclasses of K_ATP channels exist in various tissue types due to the unique assemblies of specific pore-forming (Kir6.x) and accessory (SURx) subunits. The majority of pharmacological openers and blockers act by binding to SURx and are poorly selective against the various K_ATP channel subclasses. Methods and Results: We used 3D models of the Kir6.2/SUR homotetramers based on existing cryo-EM structures of channels in both the open and closed states to identify a potential agonist binding pocket in a functionally critical area of the channel. C

SUBMITTER: Gando I 

PROVIDER: S-EPMC10319115 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature