Article
Glibenclamide binding to sulphonylurea receptor subtypes: dependence on adenine nucleotides.
British journal of pharmacology - 1 Aug 2002
Hambrock Annette, Löffler-Walz Cornelia, Quast Ulrich
Abstract excerpt
1: ATP-sensitive K(+) channels are composed of pore-forming subunits Kir6.2 and of sulphonylurea receptors (SURs); the latter are the target of the hypoglycaemic sulphonylureas like glibenclamide. Here, we report on the negative allosteric modulation by MgATP and MgADP of glibenclamide binding to SUR1 and to SUR2 mutants with high glibenclamide affinity, SUR2A(Y1206S) and SUR2B(Y1206S). 2: ATP, in the presence of...
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