ATP-sensitive potassium channel subunit Kir6.2 and sulfonylurea receptor 1 (Pancreatic β-cell KATP channel) (KATP channel)

The pancreatic β-cell KATP channel is a metabolic sensor that couples intracellular ATP/ADP ratios to membrane excitability, composed of four Kir6.2 (inward-rectifier potassium channel) subunits and four SUR1 (sulfonylurea receptor 1) subunits, forming a hetero-octameric ion channel complex. In pancreatic β-cells, closure of this channel in response to rising ATP levels from glucose metabolism leads to membrane depolarization, opening of voltage-gated calcium channels, and subsequent insulin secretion. Mutations in Kir6.2 or SUR1 can cause neonatal diabetes (gain of function) or congenital hyperinsulinism (loss of function), making KATP channels a major therapeutic target for antidiabetic agents such as sulfonylureas and diazoxide. Multiple drugs interact with the channel by either blocking or activating it, critically influencing β-cell function and glucose homeostasis[1][4][5][7].

Other names

ATP-sensitive potassium channelβ-cell KATP channelKir6.2/SUR1 channelKATPKir6.2/SUR1ATP-sensitive K+ channel

Inhibition (closing) of KATP channels stimulates insulin secretion by depolarizing β-cells (sulfonylureas, meglitinides)[1][2][5] Opening of KATP channels hyperpolarizes cells and suppresses insulin secretion (diazoxide)[7][4]