Met-204 and Tyr-205 are together important for binding GLP-1 receptor agonists but not their N-terminally truncated analogues |
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Authors: | López de Maturana Rakel Treece-Birch Janet Abidi Fatima Findlay John B C Donnelly Dan |
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Affiliation: | Faculty of Biological Sciences, University of Leeds, Leeds LS2 9JT, UK. |
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Abstract: | A mutagenesis study to systematically analyse residues spanning the first extracellular loop of the GLP-1 receptor identified a double mutant, Met-204/Tyr-205-Ala/Ala, which displayed: markedly reduced affinity for the natural agonist GLP-1; slightly reduced affinity for its analogue exendin-4; and unaltered affinity for several N-terminally truncated analogues of GLP-1 and exendin-4. This suggests that the locus is important for the formation of the binding site for the N-terminal residues of peptide agonists. |
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