Target intelligence / Profile preview

Melanocortin Receptor Type 1 (MC1R)

Target
MC1R
Molecular classification
G protein–coupled receptor, Receptor
01

Overview

The melanocortin 1 receptor (MC1R) is a G protein–coupled receptor primarily involved in regulating skin and hair pigmentation. It controls the type of melanin (eumelanin or pheomelanin) produced by melanocytes. Activation favors eumelanin synthesis, providing UV protection, while lack of activation leads to pheomelanin production, offering less UV protection. MC1R also plays a role in immune modulation and, recently discovered, in cholesterol and bile acid metabolism in hepatocytes. Genetic variations are associated with red hair, fair skin, freckles, and increased melanoma risk due to impaired DNA repair after UV exposure.

Other names
Melanocyte-stimulating hormone receptor (MSHR)Melanotropin receptorMelanin activating peptide receptor
02

Mechanism of action

Activation increases cAMP signaling, leading to upregulation of melanin production and enhanced nucleotide excision repair.

03

Biological functions

Signal transductionRegulation of melanogenesisImmune modulationRegulation of cholesterol metabolismRegulation of bile acid metabolismDNA repair
04

Disease associations

Pigmentation disordersMelanoma susceptibilityHypercholesterolemiaLiver fibrosisInflammation
05

Safety considerations

Increased melanoma risk with loss-of-function variantsIncreased sensitivity to sunlight with loss-of-function variants
06

Interacting drugs

α-MSH

2 more in the full profile.

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