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ID: ALA1131909

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.

Authors: Burden JE, Davis P, Porreca F, Spatola AF.

Abstract: Tyr-c[D-Lys-Phe-Ala], YKFA, is a potent opioid peptide analog with subnanomolar IC50s toward mu and delta receptors. Transposing Phe and Tyr, a modification found to promote mu antagonist activity in opioid/somatostatin hybrids, gave surprisingly high mu agonist activities for several related analogs, considering the lack of a 1-position hydroxyl function.

CiteXplore: 10617088

DOI: 10.1016/s0960-894x(99)00625-3