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

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.

SUBMITTER: Carotenuto A

PROVIDER: S-EPMC5070805 | biostudies-literature | 2015 Dec

REPOSITORIES: biostudies-literature

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

Carotenuto Alfonso A Merlino Francesco F Cai Minying M Brancaccio Diego D Yousif Ali Munaim AM Novellino Ettore E Hruby Victor J VJ Grieco Paolo P

Journal of medicinal chemistry 20151216 24

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 sel ...[more]

PMID: 26599352

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