Target intelligence / Profile preview

Corticotropin-Releasing Factor Type 2 Receptor (CRFR2)

Target
CRFR2
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Corticotropin-releasing factor type 2 receptor (CRFR2) is a G protein-coupled receptor that binds corticotropin-releasing hormone (CRH) and related peptides such as urocortin II and urocortin III. It plays roles in stress response modulation, angiogenesis, and energy homeostasis. Expressed in both the central nervous system and peripheral tissues, CRFR2 is a therapeutic target for psychiatric disorders and other conditions. Activation inhibits VEGF release from SMCs, SMC proliferation, capillary tube formation, and retards cell cycle progression via retinoblastoma protein downregulation. Heterodimerization between CRFR1 and CRFR2 increases cell surface expression of CRFR2.

Other names
CRHR2CRF-RBCRF2HM-CRFCorticotropin-releasing hormone receptor 2
02

Mechanism of action

Agonism or antagonism of CRFR2 modulates downstream signaling pathways via G proteins and adenylate cyclase, affecting cAMP levels and cellular function.

03

Biological functions

Signal transductionStress response modulationRegulation of angiogenesisEnergy homeostasis
04

Disease associations

Psychiatric disorders (e.g., anxiety, PTSD)Cardiovascular disease (angiogenesis)Metabolic disorders
05

Safety considerations

Potential for complex and diverse effects due to widespread tissue distribution.Chronic activation can promote anxiety-like states.

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