PathHunter® eXpress CCKAR Activated GPCR Internalization Assay

Background Information:

The PathHunter® CCKAR 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. cholecystokinin) based internalization of CCKAR 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 CCKAR. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting CCKAR-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:

Cholecystokinin

Sub Family:

Class A

Coupling:

Gq

Protein Name:

CCK1 (CCKA)

Protein Aliases:

CCK-AR|Cholecystokinin-1 receptor|CCK1-R

Accession Number:

AY322549

UniProt Number:

P32238

Gene Name:

CCKAR

Gene ID:

886

Target Species:

Human

Cell Background:

U2OS