+ Site Statistics
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

High-throughput screening using beta-lactamase reporter-gene technology for identification of low-molecular-weight antagonists of the human gonadotropin releasing hormone receptor



High-throughput screening using beta-lactamase reporter-gene technology for identification of low-molecular-weight antagonists of the human gonadotropin releasing hormone receptor



Assay and Drug Development Technologies 3(2): 143-154



G- protein coupled receptors ( GPCRs) signal via G- proteins to intracellular second messengers. Assays that link transcription of a detectable reporter to promoters that are activated by such signaling cascades are highly sensitive and allow screening for compounds that either activate or inactivate a GPCR of interest. This study describes the development and performance of an antagonistic screen on the human gonadotropin releasing hormone receptor ( GnRH- R).

Please choose payment method:






(PDF emailed within 0-6 h: $19.90)

Accession: 012151158

Download citation: RISBibTeXText

PMID: 15871689

DOI: 10.1089/adt.2005.3.143


Related references

A phenotypic high throughput screening assay for the identification of pharmacoperones for the gonadotropin releasing hormone receptor. Assay and Drug Development Technologies 12(4): 238-246, 2015

Development of an intact cell reporter gene beta-lactamase assay for G protein-coupled receptors for high-throughput screening. Analytical Biochemistry 314(1): 16-29, 2003

A short-incubation reporter-gene assay for high-throughput screening of estrogen receptor-alpha antagonists. Assay and Drug Development Technologies 3(4): 393-400, 2005

Identification and characterization of the gonadotropin-releasing hormone response elements in the mouse gonadotropin-releasing hormone receptor gene. Journal of Biological Chemistry 274(2): 867-880, 1999

Cellular LanthaScreen and beta-lactamase reporter assays for high-throughput screening of JAK2 inhibitors. Assay and Drug Development Technologies 6(4): 519-529, 2008

The promoter of the rat gonadotropin-releasing hormone receptor gene directs the expression of the human placental alkaline phosphatase reporter gene in gonadotrope cells in the anterior pituitary gland as well as in multiple extrapituitary tissues. Endocrinology 145(2): 983-993, 2003

Application of beta-galactosidase enzyme complementation technology as a high throughput screening format for antagonists of the epidermal growth factor receptor. Journal of Biomolecular Screening 6(6): 401-411, 2002

Negative regulation of gonadotropin-releasing hormone and gonadotropin-releasing hormone receptor gene expression by a gonadotropin-releasing hormone agonist in the rat hypothalamus. Journal of Neuroendocrinology 11(3): 195-201, 1999

Molecular structure of the human gonadotropin-releasing hormone receptor gene. European Journal of Endocrinology 137(2): 183-192, 1997

Identification of an upstream promoter in the human gonadotropin-releasing hormone receptor gene. Biochemical and Biophysical Research Communications 270(3): 766-772, 2000

Radiation inactivation (target size analysis) of the gonadotropin-releasing hormone receptor: evidence for a high molecular weight complex. Endocrinology 116(4): 1324-1326, 1985

Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists. Journal of Medicinal Chemistry 46(11): 2023-2026, 2003

Gonadotropin releasing hormone stimulation of gonadotropin release from the pituitary regulation of cell responses and gonadotropin releasing hormone receptors by gonadotropin releasing hormone receptor micro aggregation. Journal of Cellular Biochemistry Supplement (8 PART A): 233, 1984

Functional characterization of cell lines for high-throughput screening of human neuromedin U receptor subtype 2 specific agonists using a luciferase reporter gene assay. European Journal of Pharmaceutics and Biopharmaceutics 67(1): 284-292, 2007

A chicken gonadotropin-releasing hormone receptor that confers agonist activity to mammalian antagonists. Identification of D-Lys(6) in the ligand and extracellular loop two of the receptor as determinants. Journal of Biological Chemistry 276(11): 7754-7761, 2000