TY - JOUR
T1 - Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor
AU - Carotenuto, Alfonso
AU - Merlino, Francesco
AU - Cai, Minying
AU - Brancaccio, Diego
AU - Yousif, Ali Munaim
AU - Novellino, Ettore
AU - Hruby, Victor J.
AU - Grieco, Paolo
N1 - Funding Information:
This work was supported in part by a grant from the US Public Health Service, NIH IRO12M108040 and Italian grant, MIUR, PRIN2011, 2010MCLBCZ-002.
Publisher Copyright:
© 2015 American Chemical Society.
PY - 2015/12/24
Y1 - 2015/12/24
N2 - 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.
AB - 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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U2 - 10.1021/acs.jmedchem.5b01285
DO - 10.1021/acs.jmedchem.5b01285
M3 - Article
C2 - 26599352
AN - SCOPUS:84953257410
VL - 58
SP - 9773
EP - 9778
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 24
ER -