Target intelligence / Profile preview

Melanocortin Receptor 2 (MC2R)

Target
MC2R
Molecular classification
G protein-coupled receptor, GPCR, Melanocortin receptor, Class A Rhodopsin-like GPCR
01

Overview

Melanocortin receptor 2 (MC2R), also known as the adrenocorticotropic hormone receptor (ACTHR), is a G protein-coupled receptor (GPCR) that mediates the effects of adrenocorticotropic hormone (ACTH). It is primarily expressed in the adrenal cortex, where it plays a critical role in steroidogenesis, specifically glucocorticoid synthesis and secretion. Functional expression requires co-expression with MRAP (Melanocortin 2 Receptor Accessory Protein).

Other names
ACTHRAdrenocorticotropic Hormone ReceptorMelanocortin 2 Receptor
02

Mechanism of action

Agonist binding activates adenylyl cyclase via Gs proteins, increasing intracellular cAMP levels, leading to activation of protein kinase A (PKA) and subsequent stimulation of glucocorticoid production.

03

Biological functions

Signal transductionSteroidogenesisGlucocorticoid synthesisRegulation of adrenal cortex functioncAMP signaling pathway
04

Disease associations

Familial glucocorticoid deficiencyCushing syndrome
05

Safety considerations

Potential for adrenal insufficiency upon cessation of ACTH analogsRisk of hyperpigmentation due to cross-reactivity with other MCRs in cases of elevated ACTH levels
06

Interacting drugs

ACTH

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