1: Mini Rev Med Chem. 2002 Dec;2(6):565-72.


Structure-activity relationship, conformation and pharmacology studies of morphiceptin analogues--selective mu-opioid receptor ligands.

Janecka A, Fichna J, Mirowski M, Janecki T.

Department of Medicinal Chemistry, Medical University of Lodz, 90-131 Lodz, Poland. ajanecka@csk.am.lodz.pl

Morphiceptin (Tyr-Pro-Phe-Pro-NH(2)) is one of the most selective agonists for the mu-opioid receptor. In this review structure-activity relationships of morphiceptin analogues and studies resulting in defining low energy conformations are discussed. Finally, new developments in the control of tumour growth and cell proliferation by morphiceptin analogues are surveyed, which open future perspectives in the diagnosis and treatment of various cancers.

Publication Types:
Review

PMID: 12370041 [PubMed - indexed for MEDLINE]

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2: Masui. 1996 Sep;45(9):1060-66.


[Molecular biological study on structure and function of the opioid receptor]

[Article in Japanese]

Fukuda K.

Department of Anesthesia, Kyoto University Hospital.

Pharmacological actions of opioid analgesics are mediated by the mu-, delta- and kappa-opioid receptors in the nervous system. To understand the molecular basis of the opioid receptor functions, experiments using molecular biological methods have been performed. Amino acid sequences elucidated by cDNA cloning revealed that the opioid receptor possesses characteristic structural features of the G-protein-coupled receptor family, including the presence of seven transmembrane segments. Furthermore, molecular mechanism for the ligand selectivity of the mu- and delta-opioid receptors was investigated by analyzing chimeric receptors between the mu- and delta-receptors and mutant receptors with one amino acid replacement.

Publication Types:
English Abstract
Review

PMID: 8905940 [PubMed - indexed for MEDLINE]