PathHunter® eXpress CALCR-RAMP1 (AMY1) β-Arrestin Recruitment Assay (CHO-K1)

Background Information:

The PathHunter® CALCR-RAMP1 (AMY1) Beta Arrestin 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 alongside modulator protein RAMP1 and EA-tagged β-Arrestin-2. 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.
Amylin receptors (AMY1, AMY2, AMY3) can be activated by both amylin and calcitonin. Amylin itself is a 37–amino acid peptide hormone produced mainly in pancreatic β-cells, where it is co-released with insulin following nutrient intake. Structurally, amylin receptors belong to the GPCR family and consist of the calcitonin receptor (a seven-transmembrane protein) partnered with one of three receptor activity-modifying proteins (RAMP1–3). Therapeutically, compounds that act as dual agonists of the amylin and calcitonin receptors have demonstrated strong effects on body weight reduction, improved glucose regulation, and decreased hepatic fat accumulation. In addition, while amylin and GLP-1 receptor agonists share overlapping functions in appetite regulation, they operate through distinct mechanisms. This makes amylin-targeted therapies an attractive strategy for obesity treatment.

Target Class:

GPCR

Family:

Calcitonin

Sub Family:

Class B

Coupling:

Gs

Accession Number:

NM_001742.2; NM_005855.2

Target Species:

Human

Cell Background:

CHO-K1