ATP-sensitive potassium channel (Sulfonylurea receptor 1 is the regulatory subunit, commonly called SUR1) (KATP channel (SUR1); sometimes rendered as Kir6.2/SUR1 complex)

The ATP-sensitive potassium channel is an octameric protein complex composed of four pore-forming Kir6.x subunits and four sulfonylurea receptor 1 (SUR1) regulatory subunits. The SUR1 subunit is a member of the ATP-binding cassette (ABC) transporter family and functions as a regulatory module, conferring sensitivity to metabolites (ATP/ADP), channel openers, and inhibitors like sulfonylureas. In pancreatic beta cells, closure of the channel by ATP or drugs leads to membrane depolarization, triggering insulin release; defective function due to genetic mutations causes disorders such as neonatal diabetes or congenital hyperinsulinism. KATP channels play critical roles in energy sensing and cell excitability across diverse tissues (pancreas, brain, heart, muscle) and are established targets for anti-diabetic drugs and have emerging roles in migraine and cardiovascular disease therapy. Safety concerns primarily involve hypoglycemia from excessive inhibition and cardiovascular effects from openers or unintentional modulation.

Other names

Sulfonylurea receptor 1SUR1KATP channel (when specifically referring to the Kir6.2/SUR1 complex)Kir6.2/SUR1 channelABC transporter subfamily C member 8 (for SUR1 subunit)ATP-sensitive potassium channel, pancreatic beta-cell type

Sulfonylureas: Bind to SUR1, inhibit channel, depolarize cell membrane, stimulate insulin secretion KATP channel openers: Bind to SUR1, keep channel open, result in hyperpolarization and reduced excitability/secretion (e.g., reduced insulin secretion or vasodilation) Mutations affecting channel gating, trafficking, and assembly modify pharmacological response and disease risk