IDENTIFICATION OF THE AMINO-ACID-RESIDUES INVOLVED IN SELECTIVE AGONIST BINDING IN THE FIRST EXTRACELLULAR LOOP OF THE DELTA-OPIOID AND MU-OPIOID RECEPTORS

被引:33
作者
FUKUDA, K
TERASAKO, K
KATO, S
MORI, K
机构
[1] Department of Anesthesia, Kyoto University Hospital, Sakyo-ku, Kyoto, 606-01, 54 Kawahara-cho, Shogoin
关键词
OPIOID RECEPTOR; SITE-DIRECTED MUTAGENESIS; CDNA EXPRESSION; AGONIST-BINDING AFFINITY;
D O I
10.1016/0014-5793(95)01034-C
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Effects of amino acid substitutions in the first extracellular loop region of the delta- and mu-opioid receptors were examined. Substitution of lysine-108 of the delta-receptor (delta K108) with asparagine improved affinity to [D-Ala(2),MePhe(4),Gly-ol(5)]enk ephalin (DAGO), a mu-selective peptide agonist, to be comparable with that of the mu-receptor. On the other hand, replacement of mN127 with lysine decreased the affinity to DAGO by similar to 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 delta- and mu-receptors.
引用
收藏
页码:177 / 181
页数:5
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