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
Actions
Authors
- 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
Terms of use
- Copyright holder:
- De Wet et al
- Copyright date:
- 2015
- Notes:
- © 2015 Authors; published by Portland Press Limited
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