MISC

1995年3月

LOCATION OF REGIONS OF THE OPIOID RECEPTOR INVOLVED IN SELECTIVE AGONIST BINDING

JOURNAL OF BIOLOGICAL CHEMISTRY
  • K FUKUDA
  • ,
  • S KATO
  • ,
  • K MORI

270
12
開始ページ
6702
終了ページ
6709
記述言語
英語
掲載種別
DOI
10.1074/jbc.270.12.6702
出版者・発行元
AMER SOC BIOCHEMISTRY MOLECULAR BIOLOGY INC

To elucidate which portions of the opioid receptor molecules are involved in the ligand selectivity, we have expressed chimeric receptors between the rat delta- and mu-opioid receptors from cDNAs and analyzed their ligand binding properties, We demonstrate that the major binding determinant for the delta-selective enkephalin related peptide, [D-Pen(2),D-Pen(5)]enkephalin, resides within the region comprising the transmembrane segments V-VII and the intervening loop regions, On the other hand, the region spanning from the intracellular loop I to the amino terminal half of the transmembrane segment III is shown to be involved in determining high-affinity binding of the mu-selective enkephalin-related peptides, [D-Ala(2),MePhe(4),Gly-ol(5)]enkephalin and [D-Ala(2), MePhe(4),Met-ol(5)]enkephalin, whereas the major determinant nant for binding of the mu-selective alkaloids, morphine and codeine, is demonstrated to exist in the region spanning the transmembrane segments V-VII, These results indicate that distinct regions of the opioid receptor determine the selectivity for the delta- and the mu-selective enkephalin-related peptides and that the binding determinant for the mu-selective alkaloids is distinct from that for the mu-selective enkephalin-related peptides.

Web of Science ® 被引用回数 : 83

リンク情報
DOI
https://doi.org/10.1074/jbc.270.12.6702
CiNii Articles
http://ci.nii.ac.jp/naid/80008226118
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/7896813
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:A1995QQ85500044&DestApp=WOS_CPL

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