GNRHR binds GNRHR peptide antagonists

Stable Identifier
Reaction [binding]
Homo sapiens
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Gonadotropin-releasing hormone (GNRH) is a naturally occurring decapeptide that modulates the hypothalamic-pituitary-gonadal axis. GNHR binding to GNRH receptors causes the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which, in turn, affect the downstream synthesis and release of the sex hormones testosterone, dihydrotestosterone, estrone, and estradiol.

GNRHR peptide antagonists antagonize the GNRHR and thus the action of GNRH (Beckers et al. 1995, Beckers et al. 1997). In men, the reduction in LH leads to rapid suppression of testosterone production in the testes; in women it leads to suppression of estradiol and progesterone production from the ovaries. GNRHR peptide antagonists are used in the treatment of prostate cancer (abarelix, degaralix) (Debruyne 2004, Van Poppel 2010, Sakai et al. 2015) or female infertility in assisted reproduction (cetrorelix, ganirelix) (Diedrich et al. 2001, Al-Inany et al. 2016).
Literature References
PubMed ID Title Journal Year
7649152 Selection and characterization of mammalian cell lines with stable over-expression of human pituitary receptors for gonadoliberin

Marheineke, K, Reiländer, H, Hilgard, P, Beckers, T

Eur. J. Biochem. 1995
25811175 In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonist degarelix on human prostate cell growth

Martinez-Arguelles, DB, Sakai, M, Patterson, NH, Chaurand, P, Papadopoulos, V

PLoS One 2015
9300077 Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay

Reiländer, H, Hilgard, P, Beckers, T

Anal. Biochem. 1997
Orthologous Events
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