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