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Expression cloning of the pancreatic beta cell receptor for the gluco-incretin hormone glucagon-like peptide 1.
Open accessAbstract
Glucagon-like peptide 1 (GLP-1) is a hormone derived from the preproglucagon molecule and is secreted by intestinal L cells. It is the most potent stimulator of glucose-induced insulin secretion and also suppresses in vivo acid secretion by gastric glands. A cDNA for the GLP-1 receptor was isolated by transient expression of a rat pancreatic islet cDNA library into COS cells; this was followed by binding of radiolabeled GLP-1 and screening by photographic emulsion autoradiography. The receptor transfected into COS cells binds GLP-1 with high affinity and is coupled to activation of adenylate cyclase. The receptor binds specifically GLP-1 and does not bind peptides of related structure and similar function, such as glucagon, gastric inhibitory peptide, vasoactive intestinal peptide, or secretin. The receptor is 463 amino acids long and contains seven transmembrane domains. Sequence homology is found only with the receptors for secretin, calcitonin, and parathyroid hormone, which form a newly characterized family of G-coupled receptors.
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“Expression of the GLP-1 receptor is widely detected in various cells and organs including the kidney, lung, heart, hypothalamus, endothelial cells, neurons, astrocytes, and microglia as well as pancreatic beta-cells [12–17]”
From Anti-Inflammatory Effects of GLP-1-Based Therapies beyond Glucose Control (2016) · cites this paper as [13]
In the citing paper
“GLP-1 acts through a class 2 member of the G-coupled protein C receptor family seven-transmembrane receptor (GLP-1R) (8), which is mainly expressed in pancreatic islets, the brain, and the gastrointestinal (GI) tract (9–12), and less prominently in the kidney and eyes (11–13).”
From The science of safety: adverse effects of GLP-1 receptor agonists as glucose-lowering and obesity medications (2026) · cites this paper as [8]
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Metadata
- Authors
- Thorens, B.
- Affiliations
- University of Lausanne (CH)
- Corresponding author
- Thorens, B
- ORCID
- Thorens, B
- Venue
- Proceedings of the National Academy of Sciences
- Publisher
- National Academy of Sciences
- Published
- 1992-09-15
- Volume
- 89
- Issue
- 18
- Pages
- 8641-8645
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- PMC
- PMC49976
- OpenAlex
- W2074501705
- Cited by
- 906
- References
- 3
- Citations by year
- 2026: 21 · 2025: 19 · 2024: 28 · 2023: 16 · 2022: 23 · 2021: 30 · 2020: 23 · 2019: 29 · 2018: 18 · 2017: 18 · 2016: 25 · 2015: 26 · 2014: 41 · 2013: 36 · 2012: 32
- FWCI
- 34.79
- Type
- journal article
- Language
- en
- Open access
- green
- europepmc.org
- Locations
- Proceedings of the National Academy of Sciences (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- IRIS (submittedVersion)
- SERVAL (Université de Lausanne) (submittedVersion)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Pancreatic function and diabetes
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- glucagon-like peptide-1, GLP-1 receptor, pancreatic beta cells, expression cloning, G protein-coupled receptors, adenylate cyclase activation, insulin secretion, preproglucagon
- MeSH terms
- Glucagon-Like Peptide-1 Receptor, Animals, Base Sequence, Cloning, Molecular, DNA, Islets of Langerhans, Molecular Sequence Data, Peptides, Rats, Inbred Strains, Receptors, Cell Surface, Receptors, Gastrointestinal Hormone, RNA, Messenger, Tissue Distribution, Transfection, Gene Expression, Sequence Alignment, Receptors, Calcitonin, Receptors, Parathyroid Hormone, Receptors, Glucagon, Receptors, G-Protein-Coupled, Rats, Glucagon-Like Peptide 1
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