Identification of the amino acid residues involved in selective agonist binding in the first extracellular loop of the δ‐ and μ‐opioid receptors
- 9 October 1995
- journal article
- research article
- Published by Wiley in FEBS Letters
- Vol. 373 (2) , 177-181
- https://doi.org/10.1016/0014-5793(95)01034-c
Abstract
Effects of amino acid substitutions in the first extracellular loop region of the β- and μ-opioid receptors were examined. Substitution of lysine-108 of the δ-receptor (δK108) with asparagine improved affinity to [d-Ala2,MePhe4,Gly-ol5]enk ephalin (DAGO), a μ-selective peptide agonist, to be comparable with that of the μ-receptor. On the other hand, replacement of mN127 with lysine decreased the affinity to DAGO by ∼ 15-fold. These results suggest that dK108 and mN127, which correspond to each other in the aligned amino acid sequences, mainly determine the difference in DAGO binding affinity between the δ- and μ-receptorsKeywords
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