PKC-dependent stimulation of exocytosis by sulfonylureas in pancreatic beta cells
(1996) In Science 271(5250). p.813-815- Abstract
- Hypoglycemic sulfonylureas represent a group of clinically useful antidiabetic compounds that stimulate insulin secretion from pancreatic beta cells. The molecular mechanisms involved are not fully understood but are believed to involve inhibition of potassium channels sensitive to adenosine triphosphate (KATP channels) in the beta cell membrane, causing membrane depolarization, calcium influx, and activation of the secretory machinery. In addition to these effects, sulfonylureas also promoted exocytosis by direct interaction with the secretory machinery not involving closure of the plasma membrane KATP channels. This effect was dependent on protein kinase C (PKC) and was observed at therapeutic concentrations of sulfonylureas, which... (More)
- Hypoglycemic sulfonylureas represent a group of clinically useful antidiabetic compounds that stimulate insulin secretion from pancreatic beta cells. The molecular mechanisms involved are not fully understood but are believed to involve inhibition of potassium channels sensitive to adenosine triphosphate (KATP channels) in the beta cell membrane, causing membrane depolarization, calcium influx, and activation of the secretory machinery. In addition to these effects, sulfonylureas also promoted exocytosis by direct interaction with the secretory machinery not involving closure of the plasma membrane KATP channels. This effect was dependent on protein kinase C (PKC) and was observed at therapeutic concentrations of sulfonylureas, which suggests that it contributes to their hypoglycemic action in diabetics. (Less)
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https://lup.lub.lu.se/record/1109849
- author
- organization
- publishing date
- 1996
- type
- Contribution to journal
- publication status
- published
- subject
- in
- Science
- volume
- 271
- issue
- 5250
- pages
- 813 - 815
- publisher
- American Association for the Advancement of Science (AAAS)
- external identifiers
-
- pmid:8628999
- scopus:13344269671
- ISSN
- 1095-9203
- DOI
- 10.1126/science.271.5250.813
- language
- English
- LU publication?
- yes
- id
- fb786f9b-4b04-460f-b94b-bdb528300381 (old id 1109849)
- date added to LUP
- 2016-04-01 16:47:43
- date last changed
- 2022-03-15 03:00:41
@article{fb786f9b-4b04-460f-b94b-bdb528300381, abstract = {{Hypoglycemic sulfonylureas represent a group of clinically useful antidiabetic compounds that stimulate insulin secretion from pancreatic beta cells. The molecular mechanisms involved are not fully understood but are believed to involve inhibition of potassium channels sensitive to adenosine triphosphate (KATP channels) in the beta cell membrane, causing membrane depolarization, calcium influx, and activation of the secretory machinery. In addition to these effects, sulfonylureas also promoted exocytosis by direct interaction with the secretory machinery not involving closure of the plasma membrane KATP channels. This effect was dependent on protein kinase C (PKC) and was observed at therapeutic concentrations of sulfonylureas, which suggests that it contributes to their hypoglycemic action in diabetics.}}, author = {{Eliasson, Lena and Renström, Erik and Ammala, Carina and Berggren, Per-Olof and Bertorello, Alejandro M. and Bokvist, Krister and Chibalin, Alexander and Deeney, Jude T. and Flatt, Peter R. and Gabel, Jakob and Gromada, Jesper and Larsson, Olof and Lindstrom, Per and Rhodes, Christopher J. and Rorsman, Patrik}}, issn = {{1095-9203}}, language = {{eng}}, number = {{5250}}, pages = {{813--815}}, publisher = {{American Association for the Advancement of Science (AAAS)}}, series = {{Science}}, title = {{PKC-dependent stimulation of exocytosis by sulfonylureas in pancreatic beta cells}}, url = {{http://dx.doi.org/10.1126/science.271.5250.813}}, doi = {{10.1126/science.271.5250.813}}, volume = {{271}}, year = {{1996}}, }