ArticleThe Journal of biological chemistry2010
Spatial approximations between residues 6 and 12 in the amino-terminal region of glucagon-like peptide 1 and its receptor: a region critical for biological activity.
Article in The Journal of biological chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 37 citations in OpenAlex.
- Identification of peptide-binding sites within BSA using rapid, laser-induced covalent cross-linking combined with high-performance mass spectrometry.Journal of molecular recognition : JMR · 2018Article
- Genetically encoded photocross-linkers determine the biological binding site of exendin-4 peptide in the N-terminal domain of the intact human glucagon-like peptide-1 receptor (GLP-1R).The Journal of biological chemistry · 2017Article
- Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes.Pharmacological reviews · 2016Review
- Structural Determinants of Binding the Seven-transmembrane Domain of the Glucagon-like Peptide-1 Receptor (GLP-1R).The Journal of biological chemistry · 2016Article
- Positive Allosteric Modulation of the Glucagon-like Peptide-1 Receptor by Diverse Electrophiles.The Journal of biological chemistry · 2016Article
- A Hydrogen-Bonded Polar Network in the Core of the Glucagon-Like Peptide-1 Receptor Is a Fulcrum for Biased Agonism: Lessons from Class B Crystal Structures.Molecular pharmacology · 2016Article
- Article
- Disulfide Trapping for Modeling and Structure Determination of Receptor: Chemokine Complexes.Methods in enzymology · 2016Article
- The peptide agonist-binding site of the glucagon-like peptide-1 (GLP-1) receptor based on site-directed mutagenesis and knowledge-based modelling.Bioscience reports · 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
- Glucagon-like peptide-1 (GLP-1) analogs: recent advances, new possibilities, and therapeutic implications.Journal of medicinal chemistry · 2015Article
- Experiment-Guided Molecular Modeling of Protein-Protein Complexes Involving GPCRs.Methods in molecular biology (Clifton, N.J.) · 2015Article
- Structural and functional insights into the juxtamembranous amino-terminal tail and extracellular loop regions of class B GPCRs.British journal of pharmacology · 2014Review
- Regulation of glucose homeostasis by GLP-1.Progress in molecular biology and translational science · 2014Review
- A novel glucagon-related peptide (GCRP) and its receptor GCRPR account for coevolution of their family members in vertebrates.PloS one · 2013Article
- Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2012Article
- Ligand binding and activation of the secretin receptor, a prototypic family B G protein-coupled receptor.British journal of pharmacology · 2012Review
- The structure and function of the glucagon-like peptide-1 receptor and its ligands.British journal of pharmacology · 2012Review
- GLP-1R and amylin agonism in metabolic disease: complementary mechanisms and future opportunities.British journal of pharmacology · 2012Review
- Evolutionarily conserved residues at glucagon-like peptide-1 (GLP-1) receptor core confer ligand-induced receptor activation.The Journal of biological chemistry · 2012Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Understanding the molecular basis of natural ligand binding and activation of the glucagon-like peptide 1 (GLP1) receptor may facilitate the development of agonist drugs useful for the management of type 2 diabetes mellitus. We previously reported molecular approximations between carboxyl-terminal residues 24 and 35 within GLP1 and its receptor. In this work, we have focused on the amino-terminal region of GLP1, known to be critical for receptor activation. We developed two high-affinity, full agonist photolabile GLP1 probes having sites of covalent attachment in positions 6 and 12 of the 30-residue peptide (GLP1(7-36)). Both probes bound to the receptor specifically and covalently labeled single distinct sites. Chemical and protease cleavage of the labeled receptor identified the juxtamembrane region of its amino-terminal domain as the region of covalent attachment of the position 12 probe, whereas the region of labeling by the position 6 probe was localized to the first extracellular loop. Radiochemical sequencing identified receptor residue Tyr(145), adjacent to the first transmembrane segment, as the site of labeling by the position 12 probe, and receptor residue Tyr(205), within the first extracellular loop, as the site of labeling by the position 6 probe. These data provide support for a common mechanism for natural ligand binding and activation of family B G protein-coupled receptors. This region of interaction of peptide amino-terminal domains with the receptor may provide a pocket that can be targeted by small molecule agonists.
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