ArticleThe Journal of biological chemistry2012
Evolutionarily conserved residues at glucagon-like peptide-1 (GLP-1) receptor core confer ligand-induced receptor activation.
Article in The Journal of biological chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 23 citations in OpenAlex.
- Incretin-Based Therapies Through the Decades: Molecular Innovations and Clinical Impact.Medical sciences (Basel, Switzerland) · 2025Review
- Exploring the molecular structures that confer ligand selectivity for galanin type II and III receptors.PloS one · 2020Article
- Glucagon-like peptide 1 (GLP-1).Molecular metabolism · 2019 · on this mapReview
- Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes.Pharmacological reviews · 2016Review
- Positive Allosteric Modulation of the Glucagon-like Peptide-1 Receptor by Diverse Electrophiles.The Journal of biological chemistry · 2016Article
- Development of Spexin-based Human Galanin Receptor Type II-Specific Agonists with Increased Stability in Serum and Anxiolytic Effect in Mice.Scientific reports · 2016Article
- Functional Pairing of Class B1 Ligand-GPCR in Cephalochordate Provides Evidence of the Origin of PTH and PACAP/Glucagon Receptor Family.Molecular biology and evolution · 2015Article
- Ligand binding pocket formed by evolutionarily conserved residues in the glucagon-like peptide-1 (GLP-1) receptor core domain.The Journal of biological chemistry · 2015Article
- Polymorphisms of GLP-1 receptor gene and response to GLP-1 analogue in patients with poorly controlled type 2 diabetes.Journal of diabetes research · 2015Article
- A Novel Long-Acting Glucagon-Like Peptide-1 Agonist with Improved Efficacy in Insulin Secretion and β-Cell Growth.Endocrinology and metabolism (Seoul, Korea) · 2014Article
- Structural and functional insights into the juxtamembranous amino-terminal tail and extracellular loop regions of class B GPCRs.British journal of pharmacology · 2014Review
- A novel glucagon-related peptide (GCRP) and its receptor GCRPR account for coevolution of their family members in vertebrates.PloS one · 2013Article
- Molecular Coevolution of Neuropeptides Gonadotropin-Releasing Hormone and Kisspeptin with their Cognate G Protein-Coupled Receptors.Frontiers in neuroscience · 2012Article
- Structural and molecular conservation of glucagon-like Peptide-1 and its receptor confers selective ligand-receptor interaction.Frontiers in endocrinology · 2012Article
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) play important roles in insulin secretion through their receptors, GLP1R and GIPR. Although GLP-1 and GIP are attractive candidates for treatment of type 2 diabetes and obesity, little is known regarding the molecular interaction of these peptides with the heptahelical core domain of their receptors. These core domains are important not only for specific ligand binding but also for ligand-induced receptor activation. Here, using chimeric and point-mutated GLP1R/GIPR, we determined that evolutionarily conserved amino acid residues such as Ile(196) at transmembrane helix 2, Leu(232) and Met(233) at extracellular loop 1, and Asn(302) at extracellular loop 2 of GLP1R are responsible for interaction with ligand and receptor activation. Application of chimeric GLP-1/GIP peptides together with molecular modeling suggests that His(1) of GLP-1 interacts with Asn(302) of GLP1R and that Thr(7) of GLP-1 has close contact with a binding pocket formed by Ile(196), Leu(232), and Met(233) of GLP1R. This study may provide critical clues for the development of peptide and/or nonpeptide agonists acting at GLP1R.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.