Progress in the Development of Melanocortin Receptor Selective Ligands

Author(s): Boman G. Irani, Jerry R. Holder, Aleksandar Todorovic, Andrzej M. Wilczynski, Christine G. Joseph, Krista R. Wilson, Carrie Haskell-Luevano

Journal Name: Current Pharmaceutical Design

Volume 10 , Issue 28 , 2004

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The melanocortin pathway consists of endogenous agonists, antagonists, G-protein coupled receptors (GPCRs), and auxiliary proteins. This pathway has been identified to participate physiologically in numerous biological pathways including energy homeostasis, pigmentation, sexual function, inflammation, cardiovascular function, adrenal function, sebaceous gland lipid production, just to list a few. During this past decade, a clear link between the melanocortin-4 receptor (MC4R) and obesity, in both mice and humans via the regulation of food intake and energy homeostasis, has made this pathway the target of many academic and industrial research endeavors in attempts to develop potent and selective MC4R small molecules as anti-obesity therapeutic agents. Herein, we attempt to summarize the known proteins that constitute the melanocortin system and discuss advances in peptide and non-peptide drug discovery.

Keywords: proopiomelanocortin, melanocortin receptor agonists, msh, acth, corticotrophin releasing hormone, heparan sulfate proteoglycans

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Article Details

Year: 2004
Published on: 01 March, 2012
Page: [3443 - 3479]
Pages: 37
DOI: 10.2174/1381612043382891
Price: $65

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