Target intelligence / Profile preview

Corticotropin-releasing factor 2 receptor (CRHR2)

Target
CRHR2
Molecular classification
G protein-coupled receptor, GPCR, Type 2 GPCR
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Overview

The corticotropin-releasing factor 2 receptor (CRHR2) is a type 2 G protein-coupled receptor activated by urocortins II & III and corticotropin-releasing hormone. It plays a crucial role in stress adaptation, cardiovascular regulation, angiogenesis, and metabolic processes. Dysregulation of CRHR2 is implicated in various conditions including anxiety, PTSD, heart failure, and cancer, making it a potential therapeutic target.

Other names
CRF-RBCRF2CRFR2HM-CRF
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Mechanism of action

Activation of adenylate cyclase via Gαs, leading to increased intracellular cAMP

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Biological functions

Stress adaptation/recoveryRegulation of hypothalamic-pituitary-adrenal axisSerotonergic activity modulationInhibition of angiogenesisRegulation of feeding behaviorRegulation of lipid metabolismSignal transduction
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Disease associations

Anxiety disordersPost-traumatic stress disorder (PTSD)Chronic pain/fatigue syndromesHeart failureCardiac hypertrophyCancerIschemic cardiovascular diseases
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Safety considerations

Chronic activation can promote anxiety-like statesChronic activation can lead to maladaptive cardiac remodeling and dysfunction
06

Biomarkers

Urocortin II levels in heart failure patients

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