Cloning of the β Cell High-Affinity Sulfonylurea Receptor: a Regulator of Insulin Secretion
Abstract
Sulfonylureas are a class of drugs widely used to promote insulin secretion in the treatment of non-insulin-dependent diabetes mellitus. These drugs interact with the sulfonylurea receptor of pancreatic β cells and inhibit the conductance of adenosine triphosphate (ATP)-dependent potassium (K ATP ) channels. Cloning of complementary DNAs for the high-affinity sulfonylurea receptor indicates that it is a member of the ATP-binding cassette or traffic ATPase superfamily with multiple membrane-spanning domains and two nucleotide binding folds. The results suggest that the sulfonylurea receptor may sense changes in ATP and ADP concentration, affect K ATP channel activity, and thereby modulate insulin release.
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SUR1 regulates the activity of the Kir6.2 pore, endowing it with sensitivity to inhibitory sulfonylurea drugs, K+ channel openers such as diazoxide, and stimulatory effects of Mg-nucleotides.
“Instead, it regulates the activity of the Kir6.2 pore, endowing it with sensitivity to inhibitory sulfonylurea drugs (hence its name), to K+ channel openers such as diazoxide, and to the stimulatory effects of Mg-nucleotides (5, 232, 621, 698).”
From Pancreatic β-Cell Electrical Activity and Insulin Secretion: Of Mice and Men (2018) · cites this paper as [5]
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- Authors
- Aguilar-Bryan, L., Nichols, C. G., Wechsler, S. W., Clement, J. P., Boyd, A. E., González, G., Herrera-Sosa, H., Nguy, K., Bryan, J., & Nelson, D. A.
- Affiliations
- Departments of Cell Biology and Medicine, Baylor College of Medicine, Houston, TX 77030, USA.
- Washington University in St. Louis (US)
- Baylor College of Medicine (US)
- Venue
- Science
- Published
- 1995-04-21
- Volume
- 268
- Issue
- 5209
- Pages
- 423-426
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2148959338
- Cited by
- 1,315
- References
- 2
- Citations by year
- 2026: 7 · 2025: 10 · 2024: 10 · 2023: 16 · 2022: 20 · 2021: 18 · 2020: 11 · 2019: 22 · 2018: 23 · 2017: 23 · 2016: 20 · 2015: 30 · 2014: 25 · 2013: 30 · 2012: 34
- FWCI
- 124.75
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Science (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (1r01dk041898-01)
- National Heart, Lung, and Blood Institute (HL 45742, R01HL045742)
- National Institute of Diabetes and Digestive and Kidney Diseases (DK44311, DK 41898, R01DK044311)
- Topics
- Health Sciences › Medicine › Surgery › Pancreatic function and diabetes
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion Transport and Channel Regulation
- Keywords
- sulfonylurea receptor, pancreatic beta cells, insulin secretion, sulfonylureas, ATP-sensitive potassium channels, nucleotide binding fold, cDNA cloning, type 2 diabetes, ATP sensing
- MeSH terms
- Insulin Secretion, Adenosine Diphosphate, Adenosine Triphosphate, Amino Acid Sequence, Animals, Base Sequence, Cell Line, Cloning, Molecular, Cricetinae, Insulin, Islets of Langerhans, Molecular Sequence Data, Phosphorylation, Receptors, Drug, Sulfonylurea Compounds, Transfection, Tumor Cells, Cultured, Potassium Channels, Sequence Alignment, Protein Structure, Secondary, Protein Folding, ATP-Binding Cassette Transporters, Potassium Channels, Inwardly Rectifying, Sulfonylurea Receptors
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