PathHunter® eXpress GRPR Activated GPCR Internalization Assay

Background Information:

The PathHunter® GRPR Activated GPCR internalization eXpress kit provides an easy to-use cell based assay to study drug candidates affecting GPCR activation and internalization. This kit assesses ligand (e.g. gastrin-releasing peptide) based internalization of GRPR via detection of localization to the early endosome. This product uses EFC technology. The cells included overexpress EA-tagged β-arrestin 2 as well as a PK-tagged early endosome protein and untagged GRPR. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting GRPR-arrestin complex is internalized to the early endosome, leading to production of EFC signal. eXpress kits are a convenient, ready-to-use format which contains all materials needed to run the assay, including single-use vials of cryopreserved cells, cell plating media, detection reagent, and assay plates.

Target Class:

GPCR

Family:

Bombesin

Sub Family:

Class A

Coupling:

Gq

Protein Name:

BB2

Protein Aliases:

bombesin receptor 2

Accession Number:

NM_005314

UniProt Number:

P30550

Gene Name:

GRPR

Gene ID:

2925

Gene Aliases:

BB2|BB2R

Target Species:

Human

Cell Background:

U2OS