Building the Glucagon-Like Peptide-1 Receptor Brick by Brick: Revisiting a 1993 Diabetes Classic by Thorens et al.
Details
Serval ID
serval:BIB_94466F419EDE
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Building the Glucagon-Like Peptide-1 Receptor Brick by Brick: Revisiting a 1993 Diabetes Classic by Thorens et al.
Journal
Diabetes
ISSN
1939-327X (Electronic)
ISSN-L
0012-1797
Publication state
Published
Issued date
01/07/2024
Peer-reviewed
Oui
Volume
73
Number
7
Pages
1027-1031
Language
english
Notes
Publication types: Journal Article
Publication Status: ppublish
Publication Status: ppublish
Abstract
The glucagon-like peptide-1 receptor (GLP-1R) is a class B G protein-coupled receptor involved in the regulation of blood glucose levels and food intake. Stabilized agonists targeting GLP-1R are used in the treatment of type 2 diabetes and have recently become a breakthrough obesity therapy. Here, we revisit a classic article in Diabetes by Thorens et al. that described the cloning, sequencing, and functional expression of the human GLP-1R. The article also demonstrated that exendin4(1-39) was a full agonist of the human GLP-1R whereas exendin4(9-39) was a full antagonist. We discuss how the knowledge imparted by these studies has gone on to inform multiple strands of GLP-1R biology over the past three decades, including pharmacology, signaling, human genetics, structural biology, and chemical biology.
Keywords
Humans, Glucagon-Like Peptide-1 Receptor/agonists, Glucagon-Like Peptide-1 Receptor/metabolism, Glucagon-Like Peptide-1 Receptor/genetics, Diabetes Mellitus, Type 2/metabolism, Diabetes Mellitus, Type 2/drug therapy, Diabetes Mellitus, Type 2/genetics, Exenatide/therapeutic use, Exenatide/pharmacology, Hypoglycemic Agents/therapeutic use, Hypoglycemic Agents/pharmacology, Animals, Peptides/therapeutic use
Pubmed
Web of science
Open Access
Yes
Create date
25/06/2024 8:12
Last modification date
29/10/2024 7:21