New highly specific agonistic peptides for human melanocortin MC₁ receptor

A peptide with very high specificity for the human melanocortin MC₁ receptor identified by phage display was used as a lead for the design of new peptides. Two new peptides, MS05 and MS09, were synthesized and found to bind with sub-nanomolar affinities to the MC₁ receptor. Both these peptides showed strong agonistic activity at the MC₁ receptor. The MS05 was the most MC₁ receptor selective as it showed virtually no binding affinity for the MC₄ and MC₅ receptors and only micromolar affinity for the MC₃ receptor. The selectivity and potency of the new peptides make them potent tools for studies of MC₁ receptors, as well as novel potential candidate drugs for the treatment of inflammatory conditions. Copyright (C) 2000 Elsevier Science Inc.