Molecular action of sulphonylureas on KATP channels: a real partnership between drugs and nucleotides
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چکیده
منابع مشابه
Molecular action of sulphonylureas on KATP channels: a real partnership between drugs and nucleotides
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 inhibitor...
متن کاملCorrection: Molecular action of sulphonylureas on KATP channels: a real partnership between drugs and nucleotides.
“IC is the current in drug free solution obtained by averaging the current before and after application, IC50 is the drug concentration at which the inhibition is half maximal, h is the Hill coefficient, L is a scaling factor reflecting the difference between channel activity in control and MgATPcontaining solution (L = 1 in the absence of the nt) and a is the fraction of KATP current remaining...
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The molecular mechanisms underlying the actions of K channel openers (KCOs) on KATP channels were studied with the patch clamp technique in excised inside-out patches from frog skeletal muscle fibers. Benzopyran KCOs (levcromakalim and SR 47063) opened channels partially blocked by ATP, ADP, or ATP gamma s, with and without Mg2+, but they had no effects in the absence of internal nucleotides, e...
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Sulfonylureas, which stimulate insulin secretion from pancreatic β-cells, are widely used to treat both type 2 diabetes and neonatal diabetes. These drugs mediate their effects by binding to the sulfonylurea receptor subunit (SUR) of the ATP-sensitive K(+) (KATP) channel and inducing channel closure. The mechanism of channel inhibition is unusually complex. First, sulfonylureas act as partial a...
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A variety of direct and indirect techniques have revealed the existence of ATP-sensitive potassium (KATP) channels in the inner membranes of mitochondria. The molecular identity of these mitochondrial KATP (mitoKATP) channels remains unclear. We used a pharmacological approach to distinguish mitoKATP channels from classical, molecularly defined cardiac sarcolemmal KATP (surfaceKATP) channels en...
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ژورنال
عنوان ژورنال: Biochemical Society Transactions
سال: 2015
ISSN: 0300-5127,1470-8752
DOI: 10.1042/bst20150096