Biological Information

Background Information:

The Gonadotropin-releasing hormone receptor (GNRHR), also known as luteinizing hormone releasing hormone receptor (LHRHR), is a member of the seven-transmembrane G-Protein coupled receptor (GPCR) family. It is expressed on the surface of pituitary gonadotrope cells as well as lymphocytes, breast, ovary and prostate. GnRH (Gonadotropin-releasing hormone ), a decapeptide produced by the hypothalamus, plays an important role in the reproduction by regulating the pituitary-gonadal axis. Continuous high doses of GnRH or its super active agonists result in desensitization of the pituitary gonadotropes and a suppression of sex steroid production by the gonads (chemical castration). Based on these effects, the treatments with GnRH agonists has become widely used hormonal therapy of sex-steroid dependent tumors. It was also demonstrated that most tumor cells contain GnRH receptors, and the direct antiproliferative effects of GnRH analogs on cancer cells might be mediated through these receptors.

DiscoverX® Calcium cell lines overexpress naturally Gq coupled, wildtype GPCRs and are designed to detect calcium mobilization in response to agonist stimulation of the receptor. Signal can be detected using the Calcium No WashPLUS Detection Kit.

Family:

GPCR

Sub Family:

Gonadotrophin-Releasing Hormone

Class:

Class A

Coupling:

Gq

Protein Name:

GnRH

Uniprot Number:

P30968

Protein Aliases:

GnRH-R

Gene Name:

GNRHR

Gene ID:

2798

Gene Aliases:

LHRHR

Accession Number:

NM_000406.2

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Testing Information

Control Activator:

LHRH

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:

GnRH agonists are developed and utilized as anti-cancer agents.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA