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Melanocortin 3 receptor

Melanocortin 3 receptor (MC<sub>3</sub>R) is a protein that in humans is encoded by the gene.

Function

This gene encodes MC<sub>3</sub>R, a G-protein coupled receptor (GPCR) for melanocyte-stimulating hormone (MSH) and adrenocorticotropic hormone (ACTH) that is expressed in the brain.

MC3R regulates the timing of sexual maturation, the rate of linear growth and the accrual of lean mass, which are all energy-sensitive processes. Humans who carry loss-of-function mutations in MC3R have a later onset of puberty.

Research

Studies performed by the Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD), found that two specific polymorphisms in the MC3R gene may be associated with pediatric obesity and greater body mass because of greater energy intake. Children who were homozygous for C17A + G241A consumed approximately 38% more than those who did not contain aforementioned polymorphisms. The study concluded that these genetic variants did not affect energy expenditure.

Ligands

  • Ac-Val-Gln-(pI)DPhe-DTic-NH2, first MC<sub>3</sub> selective agonist, 100x selectivity over MC<sub>4</sub>.
  • Ac-Val-Gln-DBip-DTic-NH2, 140x selectivity over MC<sub>4</sub>.
  • Pyrrolidine bis-cyclic guanidines, non-peptide small molecule MC<sub>3</sub> agonists, good selectivity over MC<sub>4</sub> but not over MC<sub>1</sub> or MC<sub>5</sub>.
  • SHU-9119, mixed MC<sub>3</sub>/MC<sub>4</sub> antagonist.

Evolution

Paralogue

Source:

See also

References

Further reading

External links