Biological Information

Background Information:

The receptor for GHS (GHS-R) is a member of the superfamily of G-protein-coupled receptors. Ghrelin, an endogenous 28 amino acid present in the stomach, acts as a specific endogenous ligand for the GHS-R. Ghrelin has demonstrated potent and reproducible GH-releasing activity as well as significant prolactin-, ACTH- and cortisol-releasing activity. Its major physiological function may relate to energy homeostasis.

PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two enzyme fragments. The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal. PathHunter cell lines expressing Gq-coupled receptors can also be used to detect calcium mobilization.

Family:

GPCR

Sub Family:

Ghrelin

Class:

Class A

Coupling:

Gq

Protein Name:

GHSR

Uniprot Number:

Q92847

Protein Aliases:

GH-releasing peptide receptor|GHRP|Ghrelin receptor

Gene Name:

GHSR

Gene ID:

2693

Accession Number:

NM_198407

Organism:

Human

Cell Type:

U2OS

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

β-Arrestin Isoform:

β-Arrestin-1

Testing Information

Control Inhibitor:

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P

Control Activator:

ghrelin

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

Adverse / Beneficial Action:

In man, ghrelin was shown to stimulate food intake; it may also increase weight gain by reducing fat utilization.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA