Synthesis and Pharmacology of α/β(3)-Peptides Based on the Melanocortin Agonist

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ACS Med Chem Lett. 2015 Apr 8;6(5):568-72. doi: 10.1021/acsmedchemlett.5b00053. eCollection 2015.
Synthesis and Pharmacology of ?/?(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.
Singh A1, Tala SR2, Flores V3, Freeman K2, Haskell-Luevano C1.
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Abstract
The melanocortin-3 and -4 receptors are expressed in the brain and play key roles in regulating feeding behavior, metabolism, and energy homeostasis. In the present study, incorporation of ?(3)-amino acids into a melanocortin tetrapeptide template was investigated. Four linear ?/?(3)-hybrid tetrapeptides were designed with the modifications at the Phe, Arg, and Trp residues in the agonist sequence Ac-His-dPhe-Arg-Trp-NH2. The most potent mouse melanocortin-4 receptor (mMC4R) agonist, Ac-His-dPhe-Arg-?(3)hTrp-NH2 (8) showed 35-fold selectivity versus the mMC3R. The study presented here has identified a new template with heterogeneous backbone for designing potent and selective melanocortin receptor ligands.
KEYWORDS]peptidomimetics; ?/?3-peptides; ?-amino acids

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