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

Alfonso Carotenuto, Francesco Merlino, Minying Cai, Diego Brancaccio, Ali Munaim Yousif, Ettore Novellino, Victor J Hruby, Paolo Grieco

Research output: Contribution to journalArticle

11 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)9773-9778
Number of pages6
JournalJournal of Medicinal Chemistry
Volume58
Issue number24
DOIs
StatePublished - Dec 24 2015

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Carotenuto, A., Merlino, F., Cai, M., Brancaccio, D., Yousif, A. M., Novellino, E., Hruby, V. J., & Grieco, P. (2015). Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. Journal of Medicinal Chemistry, 58(24), 9773-9778. https://doi.org/10.1021/acs.jmedchem.5b01285