Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor.

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Hruby VJ, Cai M, Cain JP, Mayorov AV, Dedek MM, Trivedi D

Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor.

Curr Top Med Chem. 2007;7(11):1107-19.

PubMed ID

17584128 [ View in PubMed

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Abstract

The processed products of the proopiomelanocortin gene (ACTH, alpha-MSH, beta-MSH, gamma-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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Corticotropin	Adrenocorticotropic hormone receptor	Protein	Humans	Yes	Agonist	Details