Abstract
The processed products of the proopiomelanocortin gene (ACTH, α-MSH, β-MSH, γ-MSH, etc.) interact with five melanocortin receptors, the MC1R, MC2R, MC3R, MC4R, and MC5R to modulate and control many important biological functions crucial for good health both peripherally (as hormones) and centrally (as neurotransmitters). Pivotal biological functions include pigmentation, adrenal function, response to stress, fear/flight, energy homeostasis, feeding behavior, sexual function and motivation, pain, immune response, and many others, and are believed to be involved in many disease states including pigmentary disorders, adrenal disorders, obesity, anorexia, prolonged and neuropathic pain, inflammatory response, etc. The melanocortin-3 receptor (MC3R) is found primarily in the brain and spinal cord and also in the periphery, and its biological functions are still not well understood. Here we review some of the biological functions attributed to the MC3R, and then examine in more detail efforts to design and synthesize ligands that are potent and selective for the MC3R, which might help resolve the many questions still remaining about its function. Though some progress has been made, there is still much to be done in this critical area.
Keywords: g protein-coupled receptors, mcr signaling, agouti related protein, proopiomelanocortin, melanotropin peptide analogues
Current Topics in Medicinal Chemistry
Title: Design, Synthesis and Biological Evaluation of Ligands Selective for the Melanocortin-3 Receptor
Volume: 7 Issue: 11
Author(s): Matthew M. Dedek, Devendra Trivedi, Alexander V. Mayorov, James P. Cain, Minying Cai and Victor J. Hruby
Affiliation:
Keywords: g protein-coupled receptors, mcr signaling, agouti related protein, proopiomelanocortin, melanotropin peptide analogues
Abstract: The processed products of the proopiomelanocortin gene (ACTH, α-MSH, β-MSH, γ-MSH, etc.) interact with five melanocortin receptors, the MC1R, MC2R, MC3R, MC4R, and MC5R to modulate and control many important biological functions crucial for good health both peripherally (as hormones) and centrally (as neurotransmitters). Pivotal biological functions include pigmentation, adrenal function, response to stress, fear/flight, energy homeostasis, feeding behavior, sexual function and motivation, pain, immune response, and many others, and are believed to be involved in many disease states including pigmentary disorders, adrenal disorders, obesity, anorexia, prolonged and neuropathic pain, inflammatory response, etc. The melanocortin-3 receptor (MC3R) is found primarily in the brain and spinal cord and also in the periphery, and its biological functions are still not well understood. Here we review some of the biological functions attributed to the MC3R, and then examine in more detail efforts to design and synthesize ligands that are potent and selective for the MC3R, which might help resolve the many questions still remaining about its function. Though some progress has been made, there is still much to be done in this critical area.
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Cite this article as:
Matthew M. Dedek , Devendra Trivedi , Alexander V. Mayorov , James P. Cain , Minying Cai and Victor J. Hruby , Design, Synthesis and Biological Evaluation of Ligands Selective for the Melanocortin-3 Receptor, Current Topics in Medicinal Chemistry 2007; 7 (11) . https://dx.doi.org/10.2174/156802607780906654
DOI https://dx.doi.org/10.2174/156802607780906654 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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