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Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2015-12-16 00:00:00 , DOI: 10.1021/acs.jmedchem.5b01285
Alfonso Carotenuto 1 , Francesco Merlino 1 , Minying Cai 2 , Diego Brancaccio 1 , Ali Munaim Yousif 1 , Ettore Novellino 1 , Victor J. Hruby 2 , Paolo Grieco 1, 3
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2015-12-16 00:00:00 , DOI: 10.1021/acs.jmedchem.5b01285
Alfonso Carotenuto 1 , Francesco Merlino 1 , Minying Cai 2 , Diego Brancaccio 1 , Ali Munaim Yousif 1 , Ettore Novellino 1 , Victor J. Hruby 2 , Paolo Grieco 1, 3
Affiliation
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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.
中文翻译:
在Melanocortin-3受体上发现新型强效和选择性激动剂
黑皮质素受体3和4控制能量稳态,食物摄入行为以及相关的病理生理状况。melanocortin-4受体(MC4R)已得到广泛研究。相反,由于已知MC3R选择性配体的数量有限,因此缺乏与黑皮质素3受体(MC3R)的生理作用有关的知识。在这里,我们报告设计,合成,生物活性,构象分析,并与人类MC3受体的两个有效和选择性激动剂的受体对接。
更新日期:2015-12-16
中文翻译:
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在Melanocortin-3受体上发现新型强效和选择性激动剂
黑皮质素受体3和4控制能量稳态,食物摄入行为以及相关的病理生理状况。melanocortin-4受体(MC4R)已得到广泛研究。相反,由于已知MC3R选择性配体的数量有限,因此缺乏与黑皮质素3受体(MC3R)的生理作用有关的知识。在这里,我们报告设计,合成,生物活性,构象分析,并与人类MC3受体的两个有效和选择性激动剂的受体对接。