2. Academic Validation
  3. Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor

Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor

  • J Med Chem. 2015 Dec 24;58(24):9773-8. doi: 10.1021/acs.jmedchem.5b01285.
Alfonso Carotenuto 1,  Francesco Merlino 1,  Minying Cai 2,  Diego Brancaccio 1,  Ali Munaim Yousif 1,  Ettore Novellino 1,  Victor J Hruby 2,  Paolo Grieco 1 3
Affiliations

Affiliations

  • 1 Dipartimento di Farmacia, Università di Napoli Federico II , Via D. Montesano, 49, 80131, Naples, Italy.
  • 2 Department of Chemistry and Biochemistry, University of Arizona , Tucson, Arizona 85721, United States.
  • 3 CIRPEB: Centro Interuniversitario di Ricerca sui Peptidi Bioattivi, University of Naples Federico II , 80134, Naples, Italy.
PMID: 26599352 DOI: 10.1021/acs.jmedchem.5b01285
Abstract

The melanocortin receptors 3 and 4 control energy homeostasis, food-intake behavior, and correlated pathophysiological conditions. The melanocortin-4 receptor (MC4R) has been broadly investigated. In contrast, the knowledge related to physiological roles of the melanocortin-3 receptor (MC3R) is lacking because of the limited number of known MC3R selective ligands. Here, we report the design, synthesis, biological activity, conformational analysis, and docking with receptors of two potent and selective agonists at the human MC3 receptor.

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