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, 13 (4), 649-52

Structure-activity Relationship of Linear Peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the Human melanocortin-1 and -4 Receptors: DPhe7 and Trp9 Substitution

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Structure-activity Relationship of Linear Peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the Human melanocortin-1 and -4 Receptors: DPhe7 and Trp9 Substitution

Waleed Danho et al. Bioorg Med Chem Lett.

Abstract

A series of pentapeptides, based on hMC4R pentapeptide agonist (Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)), was prepared in which either DPhe(7) or Trp(9) residue was systematically substituted. A number of interesting DPhe surrogates (D-Thi, D-3-CF(3)Phe, D-2-Nal and D-3,4-diClPhe) as well as Trp surrogates (2-Nal and Bta) were identified in this study.

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