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新型强效且选择性黑素皮质素-3受体激动剂的发现。

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

作者信息

Carotenuto Alfonso, Merlino Francesco, Cai Minying, Brancaccio Diego, Yousif Ali Munaim, Novellino Ettore, Hruby Victor J, Grieco Paolo

机构信息

Dipartimento di Farmacia, Università di Napoli Federico II , Via D. Montesano, 49, 80131, Naples, Italy.

Department of Chemistry and Biochemistry, University of Arizona , Tucson, Arizona 85721, United States.

出版信息

J Med Chem. 2015 Dec 24;58(24):9773-8. doi: 10.1021/acs.jmedchem.5b01285. Epub 2015 Dec 16.

DOI:10.1021/acs.jmedchem.5b01285
PMID:26599352
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5070805/
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.

摘要

黑皮质素受体3和4控制能量平衡、食物摄入行为以及相关的病理生理状况。黑皮质素-4受体（MC4R）已得到广泛研究。相比之下，由于已知的MC3R选择性配体数量有限，关于黑皮质素-3受体（MC3R）生理作用的知识尚显匮乏。在此，我们报告了两种强效且选择性的人MC3受体激动剂的设计、合成、生物活性、构象分析以及与受体的对接情况。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/afe3/5070805/1bb6e3a1c2cc/nihms822248f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/afe3/5070805/7078bb7e71fb/nihms822248f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/afe3/5070805/1bb6e3a1c2cc/nihms822248f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/afe3/5070805/7078bb7e71fb/nihms822248f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/afe3/5070805/1bb6e3a1c2cc/nihms822248f2.jpg

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