Melanocortin receptor

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Melanocortin receptors are members of the rhodopsin family of 7-transmembrane, G protein-coupled receptors.

There are five known members of the melanocortin receptor system[1] each with differing specificities for melanocortins:[2][3][4]

These receptors are inhibited by endogenous inverse agonists agouti signalling peptide and agouti-related peptide,[6] and activated by synthetic (ie: afamelanotide) and endogenous agonist melanocyte-stimulating hormones.[7]

Selective Ligands

Several selective ligands for the melanocortin receptors are known,[8][9][10][11] and some synthetic compounds have been investigated as potential tanning, anti-obesity and aphrodisiac drugs, with tanning effects mainly from stimulation of MC1,[12] while anorectic and aphrodisiac effects appear to involve both MC3 and MC4.[13] MC1, MC3 and MC4 are widely expressed in the brain, and are also thought to be responsible for effects on mood and cognition.[14][15][16][17]

Agonists

Non-selective
MC2 selective
MC3 selective
  • gamma-MSH
MC4 selective

Antagonists and inverse agonists

MC1 selective
MC4 selective
  • Agouti-related peptide (inverse agonist at both MC3 and MC4)
  • HS-014
  • HS-024
  • MCL-0042[18]
  • MCL-0129[19]
  • MPB-10
  • SHU-9119 (agonist at MC1 and MC5, antagonist at MC3 and MC4)

References

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External links

de:Melanocortinrezeptor
  1. Melanocortins and the Melanocortin Receptor
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  5. Farooqi IS, Keogh JM, Yeo GS, Lank EJ, Cheetham T, O'Rahilly S (2003). "Clinical spectrum of obesity and mutations in the melanocortin 4 receptor gene". N. Engl. J. Med. 348 (12): 1085–95. doi:10.1056/NEJMoa022050. PMID 12646665. 
  6. Chai B, Pogozheva I, Lai Y, Li J, Neubig R, Mosberg H, Gantz I (2005). "Receptor-antagonist interactions in the complexes of agouti and agouti-related protein with human melanocortin 1 and 4 receptors". Biochemistry. 44 (9): 3418–31. doi:10.1021/bi0478704. PMID 15736952. 
  7. Pogozheva I, Chai B, Lomize A, Fong T, Weinberg D, Nargund R, Mulholland M, Gantz I, Mosberg H (2005). "Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists". Biochemistry. 44 (34): 11329–41. doi:10.1021/bi0501840. PMC 2532597Freely accessible. PMID 16114870. 
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  9. Wilson KR, Todorovic A, Proneth B, Haskell-Luevano C (2006). "Overview of endogenous and synthetic melanocortin peptides". Cellular and Molecular Biology (Noisy-le-Grand, France). 52 (2): 3–20. PMID 16914082. 
  10. Hruby VJ, Cai M, Cain JP, Mayorov AV, Dedek MM, Trivedi D (2007). "Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor". Current Topics in Medicinal Chemistry. 7 (11): 1107–19. doi:10.2174/156802607780906645. PMC 2274922Freely accessible. PMID 17584128. 
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  13. King SH, Mayorov AV, Balse-Srinivasan P, Hruby VJ, Vanderah TW, Wessells H (2007). "Melanocortin receptors, melanotropic peptides and penile erection". Current Topics in Medicinal Chemistry. 7 (11): 1098–1106. PMC 2694735Freely accessible. PMID 17584130. 
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