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

doi:10.1021/acs.jmedchem.5b01285

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

Chemistry and Biochemistry

Research output: Contribution to journal › Article

11 Citations (Scopus)

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 language	English (US)
Pages (from-to)	9773-9778
Number of pages	6
Journal	Journal of Medicinal Chemistry
Volume	58
Issue number	24
DOIs	https://doi.org/10.1021/acs.jmedchem.5b01285
State	Published - Dec 24 2015

Fingerprint

Receptor, Melanocortin, Type 3

Receptor, Melanocortin, Type 4

Homeostasis

Eating

Ligands

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

Cite this

Carotenuto, A., Merlino, F., Cai, M., Brancaccio, D., Yousif, A. M., Novellino, E., ... 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

Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. / Carotenuto, Alfonso; Merlino, Francesco; Cai, Minying; Brancaccio, Diego; Yousif, Ali Munaim; Novellino, Ettore; Hruby, Victor J; Grieco, Paolo.

In: Journal of Medicinal Chemistry, Vol. 58, No. 24, 24.12.2015, p. 9773-9778.

Research output: Contribution to journal › Article

Carotenuto, A, Merlino, F, Cai, M, Brancaccio, D, Yousif, AM, Novellino, E, Hruby, VJ & Grieco, P 2015, 'Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor', Journal of Medicinal Chemistry, vol. 58, no. 24, pp. 9773-9778. https://doi.org/10.1021/acs.jmedchem.5b01285

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

Carotenuto, Alfonso ; Merlino, Francesco ; Cai, Minying ; Brancaccio, Diego ; Yousif, Ali Munaim ; Novellino, Ettore ; Hruby, Victor J ; Grieco, Paolo. / Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. In: Journal of Medicinal Chemistry. 2015 ; Vol. 58, No. 24. pp. 9773-9778.

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Access to Document

10.1021/acs.jmedchem.5b01285