PathHunter® CHO-K1 CALCR-RAMP3 (AMY3) β-Arrestin Cell Line

Background Information:

The PathHunter® CALCR-RAMP3(AMY3) cell line is a stable, engineered cell line for use in studying drug candidates (small molecules or biologics) targeting GPCRs. This cell line enables assessment of ligand (e.g. calcitonin, amylin) based activation of CALCR GPCR activity via detection of β-arrestin recruitment. This product uses EFC technology. The included cell line overexpresses PK-tagged CALCR and EA-tagged β-Arrestin 2. Activation of CALCR stimulates the recruitment of β-Arrestin 2 and produces EFC signal. This stable modified cell line is provided as two vials of cryopreserved cells.

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 3, AMY3

Accession Number:

NM_001742.2; NM_001164737; NM_001164738

UniProt Number:

P30988

Gene Name:

CALCR

Gene ID:

799

Gene Aliases:

CTR

Target Species:

Human

Cell Background:

CHO-K1