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Sulphonylureas stimulate insulin secretion from pancreatic β-cells primarily by closing ATP-sensitive K(+) channels in the β-cell plasma membrane. The mechanism of channel inhibition by these drugs is unusually complex. As direct inhibitors of channel activity, sulphonylureas act only as partial antagonists at therapeutic concentrations. However, they also exert an additional indirect inhibitory effect via modulation of nucleotide-dependent channel gating. In this review, we summarize current knowledge and recent advances in our understanding of the molecular mechanism of action of these drugs.

Original publication




Journal article


Biochem Soc Trans

Publication Date





901 - 907


ABCC8, KATP channels, Kir6.2, SUR1, diabetes, Adenosine Triphosphate, Diabetes Mellitus, Humans, Infant, Newborn, Insulin, Ion Channel Gating, Islets of Langerhans, KATP Channels, Membrane Potentials, Sulfonylurea Compounds