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Kir6.2 is the pore-forming subunit of the ATP-sensitive potassium (KATP) channel, a crucial ion channel that links cellular metabolism to membrane potential in various tissues. It plays a key role in regulating insulin secretion, modulating action potential duration, and regulating neuronal excitability. Mutations in the KCNJ11 gene, which encodes Kir6.2, are associated with several human diseases, including neonatal diabetes mellitus and congenital hyperinsulinism. It is a target for sulfonylureas and potassium channel openers.
Sulfonylureas block Kir6.2-containing KATP channels, leading to membrane depolarization and insulin release. Potassium channel openers activate Kir6.2-containing KATP channels, leading to membrane hyperpolarization.
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