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Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2
Yanfeng Gao1, Xin Liu, Jie Wei
1Department of Biochemistry and Molecular Biology, School of Life Sciences, Lanzhou University, Lanzhou 730000, China.
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.
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