Target intelligence / Profile preview

Adrenocorticotropic Hormone Receptor (ACTHR)

Target
ACTHR
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The adrenocorticotropic hormone receptor (ACTHR), also known as melanocortin 2 receptor (MC2R), is a G protein-coupled receptor primarily expressed in the adrenal cortex. It is highly specific for its endogenous ligand, adrenocorticotropic hormone (ACTH), and plays a central role in regulating adrenal steroidogenesis. Mutations or dysfunctions associated with MC2R can lead to familial glucocorticoid deficiency type 1. Long-term overstimulation can contribute to Cushing's syndrome-like symptoms if used therapeutically.

Other names
ACTH ReceptorMelanocortin 2 ReceptorMC2R
02

Mechanism of action

ACTH binding activates Gs protein, leading to increased cAMP, PKA activation, and ultimately, increased steroidogenic enzyme expression and glucocorticoid synthesis.

03

Biological functions

Signal transductionSteroidogenesis regulationGlucocorticoid synthesis and secretionAdenylyl cyclase activationcAMP productionLipolysis stimulation
04

Disease associations

Familial Glucocorticoid Deficiency Type 1Cushing's syndrome (potential, due to overstimulation)
05

Safety considerations

Fluid retentionCardiovascular complications (due to excess glucocorticoids/mineralocorticoids)Cushing's syndrome-like symptoms (with chronic overstimulation)
06

Interacting drugs

ACTH

1 more in the full profile.

07

Biomarkers

ACTH levels (diagnostic for receptor dysfunction)Cortisol levels (assessment of receptor activity)

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