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Modification of the -MSH structure, including replacement of the oxidizable L-methionine with isosteric L-norleucine, replacement of L-phenylalanine with its enantiomer D-phenylalanine, and locking of the linear peptide sequence in its biologically active conformation by lactamization of the lysine -amino group and glutamic acid -carboxy group, led to a cyclic pseudopeptide analog of -MSH with good metabolic stability and exceptional activity, known as melanotan II ( 2 ) (Figure 1)