Biological Information
Background Information:
The gonadotropin- The Gonadotropin-releasing hormone receptor (GNRHR), also known as leutinizing 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.
Family:
GPCR
Sub Family:
Gonadotrophin-Releasing Hormone
Class:
Class A
Protein Name:
GnRH
Uniprot Number:
P30968
Protein Aliases:
GnRH-R
Gene Name:
GNRHR
Gene ID:
2798
Gene Aliases:
LHRHR
Accession Number:
NM_000406
Organism:
Human
Construct Details:
Recombinant
Cell Type:
Chem-1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
Fluorimetry
Measured Response:
Fluorescence
Testing Information
Incubation:
RT
Control Inhibitor:
Cetrorelix
Control Activator:
LHRH (3 nM)
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 70 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL testing. 2) Dose Response: 90 µL of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
16
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Adverse / Beneficial Action:
GnRH agonists are developed and utilized as anti-cancer agents.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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