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

Authors :
Carotenuto A
Merlino F
Cai M
Brancaccio D
Yousif AM
Novellino E
Hruby VJ
Grieco P
Source :
Journal of medicinal chemistry [J Med Chem] 2015 Dec 24; Vol. 58 (24), pp. 9773-8. Date of Electronic Publication: 2015 Dec 16.
Publication Year :
2015

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.

Details

Language :
English
ISSN :
1520-4804
Volume :
58
Issue :
24
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
26599352
Full Text :
https://doi.org/10.1021/acs.jmedchem.5b01285