title: Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.
abstract: Endomorphin-2 (Tyr-Pro-Phe-Phe-NH(2)) is a putative endogenous mu-opioid receptor ligand. To develop potent analgesics with less side effects related to it, we used the methods of dimerization and C-terminal modification. Through dimerization we got the 'balanced agonists' with potent analgesic activity and we have developed the structure-activity relationship between the selectivity and the distance of the two tyrosine pharmacophores. Modification at the C-terminal increased the selectivity of endomorphin-2 to mu-opioid receptor with binding affinity conserved.
authors.affiliation: Department of Biochemistry and Molecular Biology, School of Life Sciences, Lanzhou University, Lanzhou 730000, China.
authors.forename: Yanfeng
authors.initials: Y
authors.lastname: Gao
authors.forename: Xin
authors.initials: X
authors.lastname: Liu
authors.forename: Jie
authors.initials: J
authors.lastname: Wei
authors.forename: Beibei
authors.initials: B
authors.lastname: Zhu
authors.forename: Qiang
authors.initials: Q
authors.lastname: Chen
authors.forename: Rui
authors.initials: R
authors.lastname: Wang
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D008024:Ligands; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014443:Tyrosine / Q000737:chemistry
chemical_list: D000700:Analgesics; D008024:Ligands; D009842:Oligopeptides; C105294:endomorphin 2; D014443:Tyrosine