Design of cyclic peptides with agonist activity at melanocortin receptor-4

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3723-6. doi: 10.1016/j.bmcl.2006.04.050.

Takenao Odagami ¹, Yuko Tsuda, Yuji Kogami, Hiroyuki Kouji, Yoshio Okada

Affiliations

Affiliation

1 Research Center, Pharmaceutical R&D Division, Asahi Kasei Pharma Corporation, Izunokuni 410-2321, Japan.

PMID: 16678415 DOI: 10.1016/j.bmcl.2006.04.050

Abstract

A series of cyclic pentapeptides, c(His-D-Phe-Arg-Trp-Z) (Z=omega-amino acid), were prepared and biologically evaluated. The effects of increasing alkyl chain length of omega-amino acid on the functional activities and the receptor binding affinities for human melanocortin receptors (hMC-Rs) were studied. Compound 2 was an agonist for hMC-4R with an EC50 value of 15.4 nM, which was 4.7 times more potent than that of alpha-MSH. Compound 2 also showed a 4.3-fold higher hMC-4R selectivity over hMC-1R, thus providing us with information concerning size and chemical structure of the lactam ring for the development of the agonist with hMC-4R selectivity.

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