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PKC-Dependent Stimulation of Exocytosis by Sulfonylureas in Pancreatic β Cells
Abstract
Hypoglycemic sulfonylureas represent a group of clinically useful antidiabetic compounds that stimulate insulin secretion from pancreatic β cells. The molecular mechanisms involved are not fully understood but are believed to involve inhibition of potassium channels sensitive to adenosine triphosphate (K ATP channels) in the β 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 K ATP 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.
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Citations
Cited by
Pancreatic β-Cell Electrical Activity and Insulin Secretion: Of Mice and Men
Rorsman, P., & Ashcroft, F. M. (2018) · Physiological Reviews · doi:10.1152/physrev.00008.2017 · Cited by 793
Self-citationMolecular Biology of Adenosine Triphosphate-Sensitive Potassium Channels*
Aguilar-Bryan, L., & Bryan, J. (1999) · Endocrine Reviews · doi:10.1210/edrv.20.2.0361 · Cited by 698
Regulation of Insulin Secretion in Human Pancreatic Islets
Rorsman, P., & Braun, M. (2013) · Annual Review of Physiology · doi:10.1146/annurev-physiol-030212-183754 · Cited by 599
Self-citationDefective insulin secretion and enhanced insulin action in K ATP channel-deficient mice
Miki, T., Nagashima, K., Tashiro, F., Kotake, K., Yoshitomi, H., Tamamoto, A., Gonoi, T., Iwanaga, T., Miyazaki, J.-I., & Seino, S. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.18.10402 · Cited by 502
cAMP-GEFII is a direct target of cAMP in regulated exocytosis
Ozaki, N., Shibasaki, T., Kashima, Y., Miki, T., Takahashi, K., Ueno, H., Sunaga, Y., Yano, H., Matsuura, Y., Iwanaga, T., et al. (2000) · Nature Cell Biology · doi:10.1038/35041046 · Cited by 481
Metadata
- Authors
- Eliasson, L., Renström, E., Ämmälä, C., Berggren, P.-O., Bertorello, A. M., Bokvist, K., Chibalin, A., Deeney, J. T., Flatt, P. R., Gäbel, J., Gromada, J., Larsson, O., Lindström, P., Rhodes, C. J., & Rorsman, P.
- Venue
- Science
- Published
- 1996-02-09
- Volume
- 271
- Issue
- 5250
- Pages
- 813-815
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2142126460
- Cited by
- 194
- References
- 0
- FWCI
- 22.09
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: PKC-Dependent Stimulation of Exocytosis by Sulfonylureas in Pancreatic β Cells. https://app.cochat.ai/papers/10.1126/science.271.5250.813
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- Eliasson, L., Renström, E., Ämmälä, C., Berggren, P.-O., Bertorello, A. M., Bokvist, K., Chibalin, A., Deeney, J. T., Flatt, P. R., Gäbel, J., Gromada, J., Larsson, O., Lindström, P., Rhodes, C. J., & Rorsman, P. (1996). PKC-Dependent Stimulation of Exocytosis by Sulfonylureas in Pancreatic β Cells. Science. https://doi.org/10.1126/science.271.5250.813
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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