Design and Synthesis of a Novel Tetrapeptide with Improved Selectivity Towards the hMC1R

The melanocortin system plays vital roles with regard to maintaining homeostasis. The endogenous melanotropin peptides (α-, β-, γ-melanocyte stimulating hormones (MSH) are derived from the proopiomelanocortin (POMC) preprohormone gene. These melanotropin peptides all contain the same core pharmacophore amino acid sequence: His-Phe-Arg-Trp [1,2]. This sequence is important for binding to the five human melanocortin receptors (MC1R, MC2R, MC3R,...