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

Victor J Hruby, Minying Cai, James P. Cain, Alexander V. Mayorov, Matthew M. Dedek, Devendra Trivedi

Research output: Contribution to journalArticle

11 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)1107-1119
Number of pages13
JournalCurrent Topics in Medicinal Chemistry
Volume7
Issue number11
StatePublished - 2007

Fingerprint

Receptor, Melanocortin, Type 3
Ligands
gamma-MSH
beta-MSH
Melanocortin Receptors
alpha-MSH
Pro-Opiomelanocortin
Pigmentation
Anorexia
Neuralgia
Feeding Behavior
Adrenocorticotropic Hormone
Fear
Neurotransmitter Agents
Motivation
Spinal Cord
Homeostasis
Obesity
Hormones
Pain

ASJC Scopus subject areas

  • Medicine(all)
  • Chemistry(all)

Cite this

Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. / Hruby, Victor J; Cai, Minying; Cain, James P.; Mayorov, Alexander V.; Dedek, Matthew M.; Trivedi, Devendra.

In: Current Topics in Medicinal Chemistry, Vol. 7, No. 11, 2007, p. 1107-1119.

Research output: Contribution to journalArticle

Hruby, Victor J ; Cai, Minying ; Cain, James P. ; Mayorov, Alexander V. ; Dedek, Matthew M. ; Trivedi, Devendra. / Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. In: Current Topics in Medicinal Chemistry. 2007 ; Vol. 7, No. 11. pp. 1107-1119.
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