CRF1 Human Corticotropin-Releasing Factor GPCR Cell Based Agonist Activated Internalization LeadHunter Assay - US

Background Information:

Corticotropin-releasing factor (CRF, interchangeable with corticotropin-releasing hormone, CRH) receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. Two major subtypes of the CRF receptor have been termed the CRF1 and CRF2 receptors. The CRF1 receptor is abundantly expressed in the central nervous system with major expression sites in cortex, cerebellum, hippocampus, amygdala, olfactory bulb, and pituitary. CRF1 receptor antagonism may block stress-related responses and be useful in the treatment of anxiety, depression and gastrointestinal distress.

PathHunter Activated GPCR Internalization cell lines are engineered to co-express an untagged GPCR, Enzyme Acceptor (EA) tagged β-Arrestin, and a ProLink™ (PK) tag localized to the endosomes. Activation of the GPCR induces β-Arrestin recruitment, followed by internalization of the Receptor/Arrestin-EA complex in PK-tagged endosomes. This forces complementation of the two β-galactosidase enzyme fragments (EA and PK), forming functional enzyme that hydrolyzes substrate to generate a chemiluminescent signal.

Family:

GPCR

Sub Family:

Corticotropin-Releasing Factor

Class:

Class B

Coupling:

Gs

Protein Name:

CRF1

Uniprot Number:

P34998

Protein Aliases:

CRF-R1|CRFR-1|Corticotropin-releasing hormone receptor 1|CRH-R-1|CRH-R1

Gene Name:

CRHR1

Gene ID:

1394

Gene Aliases:

CRF-R|CRF1

Accession Number:

NM_001145146

Organism:

Human

Cell Type:

U2OS