New highly specific agonistic peptides for human melanocortin MC1 receptor

A peptide with very high specificity for the human melanocortin MC1 recepto r identified by phage display was used as a lead for the design of new pept ides. Two new peptides, MS05 and MS09, were synthesized and found to bind w ith sub-nanomolar affinities to the MC1 receptor. Both these peptides showe d strong agonistic activity at the MC, receptor. The MS05 was the most MC1 receptor selective as it showed virtually no binding affinity for the MC4 a nd MC5 receptors and only micromolar affinity for the MC3 receptor. The sel ectivity and potency of the new peptides make them potent tools For studies of MC1 receptors, as well as novel potential candidate drugs for the treat ment of inflammatory conditions. (C) 2000 Elsevier Science Inc. All rights reserved.