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Bioorg Med Chem Lett. 2003 Aug 18;13(16):2647-50.

Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).

Author information

1
College of Pharmacy, University of Cincinnati, Cincinnati, OH 45267, USA. lkoikov@hotmail.com

Abstract

Twenty three derivatives of the core fragment His(6)-D-Phe(7)-Arg(8)-Trp(9)-NH(2) end-capped with carboxylic and sulfonic acids were synthesized and evaluated at human melanocortin receptors (hMC1, hMC3, and hMC4Rs). The SAR within this series allowed us to map the hMCRs near the His(6) binding site and design a superpotent MC1R agonist, LK-184, Ph(CH(2))(3)CO-His-D-Phe-Arg-Trp-NH(2) (19) with EC(50) 0.01 nM (5 nM at MC3 and MC4Rs).

PMID:
12873485
DOI:
10.1016/s0960-894x(03)00552-3
[Indexed for MEDLINE]

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