GNRHR binds chemical 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.

The non-peptide GNRHR antagonist drug elagolix (Chen et al. 2008) is indicated for the treatment of moderate to severe endometriosis pain (Lamb 2018, Surrey et al. 2018, Taylor et al. 2019). The non-peptide GNRHR antagonist drug relugolix (Miwa et al. 2011) is used in the treatment of prostate cancer in men (Shore et al. 2020) and uterine fibroids in women (Barra et al. 2019). Linzagolix is a new non-peptide GNRHR antagonist under development for the treatment of uterine fibroids, endometriosis, and adenomyosis (Donnez & Donnez 2020, Donnez et al. 2020).
Literature References
PubMed ID Title Journal Year
19006286 Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor

Rowbottom, M, Saunders, J, Wu, D, Huang, CQ, Wen, J, Madan, A, Tucci, FC, Chen, C, Chen, M, Chen, Y, Zhu, YF, Wade, W, Pontillo, J, Struthers, RS, Xie, Q, Reinhart, GJ, Bozigian, H, Chen, T, Guo, Z

J. Med. Chem. 2008
21657270 Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor

Imada, T, Miwa, K, Furuya, S, Endo, S, Sasaki, S, Hamamura, K, Hitaka, T, Nakata, D, Kusaka, M, Yoshimatsu, M, Kitazaki, T, Tanaka, A

J Med Chem 2011
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