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Cited by 558

The DOI matches its Crossref record; 7 of the 7 references it cites were found in a registry or an index.

Cloning and Functional Expression of the Human Islet GLP-1 Receptor: Demonstration That Exendin-4 Is an Agonist and Exendin-(9–39) an Antagonist of the Receptor

Open access
Thorens, Bernard, Porret, Andrée, Bühler, Léo, Deng, Shao-Ping, Morel, Philippe, Widmann, Christian·1993·Diabetes

Abstract

A complementary DNA for a glucagon-like peptide-1 receptor was isolated from a human pancreatics islet cDNA library. The isolated clone encoded a protein with 90% identity to the rat receptor. In stably transfected fibroblasts, the receptor bound [125I]GLP-1 with high affinity (Kd = 0.5 nM) and was coupled to adenylate cyclase as detected by a GLP-1-dependent increase in cAMP production (EC50 = 93 pM). Two peptides from the venom of the lizard Heloderma suspectum, exendin-4 and exendin-(9–39), displayed similar ligand binding affinities to the human GLP-1 receptor. Whereas exendin-4 acted as an agonist of the receptor, inducing cAMP formation, exendin-(9–39) was an antagonist of the receptor, inhibiting GLP-1–induced cAMP production. Because GLP-1 has been proposed as a potential agent for treatment of NIDDM, our present data will contribute to the characterization of the receptor binding site and the development of new agonists of this receptor.

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Metadata

Authors
Thorens, B., Porret, A., Bühler, L., Deng, S.-P., Morel, P., & Widmann, C.
Venue
Diabetes
Published
1993-11-01
Volume
42
Issue
11
Pages
1678-1682
ISSN
  • 0012-1797 (ISSN-L)
  • 1939-327X
OpenAlex
W2142903571
Cited by
558
References
7
FWCI
7.47
Type
journal article
Language
en
Open access
bronze

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CoChat. (2026). Citation check: Cloning and Functional Expression of the Human Islet GLP-1 Receptor: Demonstration That Exendin-4 Is an Agonist and Exendin-(9–39) an Antagonist of the Receptor. https://app.cochat.ai/papers/10.2337/diab.42.11.1678
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Thorens, B., Porret, A., Bühler, L., Deng, S.-P., Morel, P., & Widmann, C. (1993). Cloning and Functional Expression of the Human Islet GLP-1 Receptor: Demonstration That Exendin-4 Is an Agonist and Exendin-(9–39) an Antagonist of the Receptor. Diabetes. https://doi.org/10.2337/diab.42.11.1678

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