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Journal article

Molecular action of sulphonylureas on KATP channels: a real partnership between drugs and nucleotides.

Abstract:
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.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1042/bst20150096

Authors


More by this author
Institution:
University of Oxford
Division:
MSD
Department:
Physiology Anatomy & Genetics
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
Physiology Anatomy & Genetics
Role:
Author


Publisher:
Portland Press Limited
Journal:
Biochemical Society transactions More from this journal
Volume:
43
Issue:
5
Pages:
901-907
Publication date:
2015-10-01
DOI:
EISSN:
1470-8752
ISSN:
0300-5127


Language:
English
Keywords:
Pubs id:
pubs:575337
UUID:
uuid:bbe12fef-aa9f-441b-90e0-5335e619f57b
Local pid:
pubs:575337
Source identifiers:
575337
Deposit date:
2015-11-26

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