The positive charge at Lys-288 of the glucagon-like peptide-1 (GLP-1) receptor is important for binding the N-terminus of peptide agonists |
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Authors: | Al-Sabah Suleiman Donnelly Dan |
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Institution: | School of Biomedical Sciences, University of Leeds, LS2 9JT, Leeds, UK. |
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Abstract: | Lysine-288 in the glucagon-like peptide-1 receptor was predicted to be ideally positioned to play a role in hormone binding. Subsequent mutation of Lys-288 to Ala or Leu greatly reduced hormone affinity, while substitution with Arg had minimal effect. Compared to wild type, the Lys288-Ala receptor had a reduced affinity for three peptide ligands with complete N-terminal sequences but not for their N-truncated analogues. Hence, the role of this positively charged residue, which is conserved at the equivalent position in all other Family B receptors, was determined to be important for receptor interaction with the N-terminal eight residues of peptide agonists. |
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Keywords: | G protein-coupled receptor Receptor Agonist Glucagon-like peptide-1 Antagonist Exendin |
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