PathHunter® eXpress CALCR-RAMP2 (AMY2) CHO-K1 β-Arrestin GPCR Assay

Background Information:

The PathHunter® CALCR-RAMP2(AMY2) eXpress kit provides an easy-to-use cell based assay to study drug candidates (small molecules or biologics) targeting GPCRs. This kit assesses ligand (e.g. calcitonin, amylin) based activation of CALCR GPCR activity via detection of β-arrestin recruitment. This product uses EFC technology. The cells included overexpress PK-tagged CALCR and EA-tagged β-Arrestin-2, along with untagged modulating protein RAMP2. Activation of CALCR stimulates the recruitment of β-Arrestin-2 and produces 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.

Both calcitonin and amylin activate amylin receptors (AMY1, AMY2, AMY3). Amylin, a 37-amino acid peptide hormone, is primarily synthesized in pancreatic beta cells and co-secreted with insulin in response to ingested nutrients. Amylin receptors are GPCRs composed of two units: a core unit formed by the calcitonin receptor (a 7-transmembrane receptor) and one of three receptor activity-modifying proteins (RAMP1-3). Dual amylin and calcitonin receptor agonists have shown significant efficacy in promoting body weight loss, enhancing glucose tolerance, and reducing fat accumulation in liver tissue. Moreover, Amylin and GLP-1R agonists are believed to function via comparable yet distinct mechanisms, particularly in regulating appetite. Consequently, Amylin-based therapeutics exhibit promising potential in combating obesity.

Target Class:

GPCR

Family:

Calcitonin

Sub Family:

Class B

Coupling:

Gs

Protein Name:

CT

Protein Aliases:

Calcitonin receptor, CRT, CT-R, CTR, CTR1, Amylin receptor 2, AMY2

Accession Number:

NM_001742.2

UniProt Number:

P30988

Gene Name:

CALCR

Gene ID:

799

Gene Aliases:

CTR

Target Species:

Human

Cell Background:

CHO-K1