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Target intelligence / Profile preview
Melanocortin type 4 receptor (MC4R)
- Target
- MC4R
- Molecular classification
- G protein-coupled receptor, GPCR, Class A GPCR, Rhodopsin-like GPCR
01
Overview
The melanocortin type 4 receptor (MC4R) is a G protein-coupled receptor (GPCR) that plays a central role in regulating appetite, energy homeostasis, and body weight. It is highly expressed in the paraventricular nucleus of the hypothalamus and other brain regions involved in energy balance. Activation of MC4R decreases food intake and increases energy expenditure. Loss-of-function mutations in MC4R are the most common monogenic cause of human obesity. Drugs targeting MC4R are under development for anti-obesity therapy.
02
Mechanism of action
Gs protein activation, cAMP increase, regulation of Kir7.1 ion channels
03
Biological functions
Regulation of appetite/feeding behaviorEnergy homeostasis/metabolismBody weight controlCardiovascular functionGlucose/lipid metabolismSexual function/reproductionSignal transduction
04
Disease associations
ObesityHyperphagiaCardiovascular diseaseMetabolic disorders
05
Interacting drugs
α-MSH
1 more in the full profile.
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