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.
Review Article| October 09 2015
Molecular action of sulphonylureas on KATP channels: a real partnership between drugs and nucleotides
Heidi de Wet;
Peter Proks 1
*Department of Physiology, Anatomy and Genetics, Le Gros Clark building, University of Oxford, South Parks Road, Oxford OX1 3QX, England, U.K.
1To whom correspondence should be addressed (email@example.com).
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Heidi de Wet, Peter Proks; Molecular action of sulphonylureas on KATP channels: a real partnership between drugs and nucleotides. Biochem Soc Trans 1 October 2015; 43 (5): 901–907. doi: https://doi.org/10.1042/BST20150096
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