Mechanism

SUR1 (short-acting)

Assets acting on this target.

Class
Meglitinide (insulin secretagogue)

SUR1, or sulfonylurea receptor 1, is a regulatory subunit that pairs with the Kir6.2 potassium channel to form the ATP-sensitive potassium (KATP) channel on pancreatic beta cells. This channel links a cell's metabolic state to its electrical activity: when the channel closes, the beta cell depolarizes, calcium enters, and insulin is released. Meglitinides are insulin secretagogues that bind SUR1 and force the KATP channel closed, prompting insulin secretion independent of the meal-driven rise in glucose metabolism that normally triggers this process. Because meglitinides associate with and dissociate from SUR1 quickly, their action is short-lived, making them suited to blunting the glucose spike that follows a meal rather than providing steady, all-day stimulation of insulin release. This mechanism is relevant wherever insulin secretion is insufficient but not absent, most notably in type 2 diabetes, where residual beta-cell capacity can be prompted to release more insulin around mealtimes. The approach requires functioning beta cells to work and depends on coordinating dosing with food intake, since the drug's effect on the channel does not last long. It sits within a broader family of SUR1-targeted secretagogues used to manage postprandial glucose control.

Research

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Company

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