Solid-phase peptide head-to-side chain cyclodimerization: Discovery of C2-symmetric cyclic lactam hybrid α-melanocyte-stimulating hormone (MSH)/agouti-signaling protein (ASIP) analogues with potent activities at the human melanocortin receptors

▶ A novel ASIP/MSH hybrid pharmacophore has been designed. ▶ A direct on-resin peptide lactam cyclodimerization is reported. ▶ Cyclodimeric ASIP/MSH hybrid peptides displayed nM range hMC1R agonist activities.