Target intelligence / Profile preview

Melanocortin Type 2 Receptor (MC2R)

Target
MC2R
Molecular classification
GPCR, G protein-coupled receptor, Melanocortin Receptors, Seven-transmembrane domain G-protein coupled receptors
01

Overview

MC2R is a G protein-coupled receptor (GPCR) that plays a critical role in the hypothalamic–pituitary–adrenal (HPA) axis, specifically mediating the effects of adrenocorticotropic hormone (ACTH). It is essential for regulating and maintaining adrenocortical function, particularly steroidogenesis—the production of glucocorticoids in the adrenal cortex. Unlike other melanocortin receptors, MC2R is unique because it binds exclusively to ACTH as its endogenous ligand. MRAP is essential for proper trafficking of MC2R from the endoplasmic reticulum to the cell membrane. Mutations in *MC2R* cause familial glucocorticoid deficiency type 1.

Other names
Adrenocorticotropic hormone receptorACTH receptorACTHR
02

Mechanism of action

Mediates steroidogenesis via cAMP/PKA pathway after binding with ACTH

03

Biological functions

Signal transductionRegulation of adrenocortical functionSteroidogenesisGlucocorticoid synthesis
04

Disease associations

Familial Glucocorticoid Deficiency type 1Familial Glucocorticoid Deficiency type 2
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Safety considerations

Familial Glucocorticoid DeficiencyInsensitivity to ACTHHypoglycemiaHyperpigmentationLifelong management required for endocrine disorders
06

Interacting drugs

ACTH

6 more in the full profile.

07

Biomarkers

ACTH levelsCortisol levels

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