PathHunter® eXpress CCR5 Activated GPCR Internalization Assay

Background Information:

The PathHunter® CCR5 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. CCL3/MIP-1α) based internalization of CCR5 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 CCR5. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting CCR5-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:

Chemokine

Sub Family:

Class A

Coupling:

Gi/Go

Protein Name:

CCR5

Protein Aliases:

CC-CKR-5|CCR-5|CCR5|CHEMR13|HIV-1 fusion coreceptor|CD antigen CD195

Accession Number:

BC038398

UniProt Number:

P51681

Gene Name:

CCR5

Gene ID:

1234

Gene Aliases:

CKR-5|CC-CKR-5|CKR5|CD195|IDDM22

Target Species:

Human

Cell Background:

U2OS