Melanocortin receptor
Melanocortin receptors are members of the
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. MC1Ris associated with pigmentation genetics.
- MC2R. MC2R is also known as the ACTH receptoror 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
- MC5R. MC5R
These receptors are
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
- BMS-470,539
- MC4-selective
- Unknown (but for certain MC2-acting)
- Alsactide
- Tetracosactide
Antagonists and inverse agonists
- Non-selective
- Agouti-related peptide
- Agouti signalling peptide
- 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
- ^ "Melanocortins and the Melanocortin Receptor". Archived from the original on 2007-04-11. Retrieved 2007-03-14.
- PMID 14535656.
- PMID 16412534.
- PMID 19456331.
- PMID 12646665.
- PMID 15736952.
- PMID 16114870.
- PMID 14584947.
- PMID 16914082.
- PMID 17584128.
- PMID 18088090.
- PMID 12851336.
- PMID 17584130.
- PMID 16325304.
- PMID 18550183.
- PMID 18625277.
- PMID 19275930.
- PMID 16337261.
- PMID 12538838.
External links
- "Melanocortin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- Melanocortin+Receptors at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
- Calculated spatial position of melanocortin-4 receptor in the lipid bilayer, inactive state with antagonist and active state with agonist