Abstract
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
Current Pharmaceutical Design
Title: Progress in the Development of Melanocortin Receptor Selective Ligands
Volume: 10 Issue: 28
Author(s): Boman G. Irani, Jerry R. Holder, Aleksandar Todorovic, Andrzej M. Wilczynski, Christine G. Joseph, Krista R. Wilson and Carrie Haskell-Luevano
Affiliation:
Keywords: proopiomelanocortin, melanocortin receptor agonists, msh, acth, corticotrophin releasing hormone, heparan sulfate proteoglycans
Abstract: 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.
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Cite this article as:
Irani G. Boman, Holder R. Jerry, Todorovic Aleksandar, Wilczynski M. Andrzej, Joseph G. Christine, Wilson R. Krista and Haskell-Luevano Carrie, Progress in the Development of Melanocortin Receptor Selective Ligands, Current Pharmaceutical Design 2004; 10 (28) . https://dx.doi.org/10.2174/1381612043382891
DOI https://dx.doi.org/10.2174/1381612043382891 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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