Melanocortin receptor
Template:Short description 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]
- MC1R. MC1R is associated with pigmentation genetics.
- MC2R. MC2R is also known as the ACTH receptor or corticotropin receptor because it is specific for ACTH alone.
- MC3R. MC3R is associated with childhood growth, accrual of lean mass and onset of puberty.[5]
- MC4R. Defects in MC4R are a cause of autosomal dominant obesity, accounting for 6% of all cases of early-onset obesity.[6]
- MC5R. MC5R
These receptors are inhibited by endogenous inverse agonists agouti signalling peptide and agouti-related peptide,[7] and activated by synthetic (i.e. afamelanotide) and endogenous agonist melanocyte-stimulating hormones.[8]
Selective ligands
Several selective ligands for the melanocortin receptors are known,[9][10][11][12] and some synthetic compounds have been investigated as potential tanning, anti-obesity and aphrodisiac drugs, with tanning effects mainly from stimulation of MC1,[13] while anorectic and aphrodisiac effects appear to involve both MC3 and MC4.[14] MC1, MC3 and MC4 are widely expressed in the brain, and are also thought to be responsible for effects on mood and cognition.[15][16][17][18]
Agonists
- Non-selective
- MC1-selective
- MC4-selective
- Unknown (but for certain MC2-acting)
Antagonists and inverse agonists
- Non-selective
- MC2-selective
- Atumelnant (CRN04894)
- MC4-selective
- HS-014
- HS-024
- MCL-0042[19]
- MCL-0129[20]
- MPB-10
- SHU-9119 (agonist at MC1 and MC5, antagonist at MC3 and MC4)
Unknown
References
External links
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- Calculated spatial position of melanocortin-4 receptor in the lipid bilayer, inactive state with antagonist and active state with agonist
Template:G protein-coupled receptors Template:Melanocortin receptor modulators
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- ↑ Lam, B.Y.H., Williamson, A., Finer, S. et al. MC3R links nutritional state to childhood growth and the timing of puberty. Nature (2021). Script error: No such module "doi".
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