Loading
The pituitary receptor that starts the hormone chain leading to testosterone and oestrogen. Agonists overstimulate it into silence and antagonists block it outright, the basis of medical castration in prostate cancer and ovarian suppression in breast cancer.
Gonadotropin-releasing hormone from the hypothalamus binds GNRHR on pituitary gonadotroph cells to release LH and FSH, which drive testicular testosterone and ovarian oestrogen production. Continuous stimulation by agonists such as leuprolide and goserelin desensitises the receptor after an initial flare, while antagonists such as degarelix and the oral relugolix block it immediately. The result is castrate testosterone in prostate cancer, the backbone of androgen deprivation therapy, and ovarian function suppression in pre-menopausal breast cancer.
In plain words · The pituitary receptor that starts the hormone chain leading to testosterone and oestrogen. Agonists overstimulate it into silence and antagonists block it outright, the basis of medical castration in prostate cancer and ovarian suppression in breast cancer.
The pituitary receptor that starts the hormone chain leading to testosterone and oestrogen. Agonists overstimulate it into silence and antagonists block it outright, the basis of medical castration in prostate cancer and ovarian suppression in breast cancer.
G protein-coupled receptor on pituitary gonadotrophs; agonist-induced desensitisation or antagonist blockade suppresses LH and FSH release.
3 products aim at GnRH receptor (GNRHR): hormonal therapies. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
Tumour-associated overexpression: HPA finds the RNA tissue enriched in normal pituitary gland, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA GNRHR: RNA tissue enriched (pituitary gland 12 nTPM); no normal tissue stained high. Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Prostate cancer, Breast cancer (all types)); approvals of single-target medicines aimed at it also list Salivary gland cancers, not counted; Open Targets associates it with 4 specific cancer types at or above 0.5 (prostate cancer, prostate carcinoma, breast cancer, uterine corpus leiomyoma). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas GNRHR tissue; Human Protein Atlas GNRHR pathology; Open Targets ENSG00000109163 associations
First described 1992. Earliest sequence paper UniProt cites for the protein: Kakar S.S. et al, Biochem. Biophys. Res. Commun, 1992, "Cloning, sequencing, and expression of human gonadotropin releasing hormone (GnRH) receptor". Source.
G protein-coupled receptor on pituitary gonadotrophs; agonist-induced desensitisation or antagonist blockade suppresses LH and FSH release.
RNA: tissue enriched (pituitary gland 12 nTPM), detected in single normal tissue.
No normal tissue stained high; medium in Pituitary gland.
No cancer sample stained medium or high.
HPA GNRHR tissue · HPA GNRHR pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Prostate cancer | host% | Host target: pituitary receptor that starts the testosterone chain. Not a tumour alteration, so no prevalence applies; the drug acts on normal tissue or on symptoms. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Abarelix was the first GnRH antagonist for prostate cancer, approved in the United States in 2003 for men who could not take agonists, but allergic reactions restricted it and it was withdrawn from the US market in 2005; it remained available in Germany.
Buserelin is one of the original GnRH agonists, approved in Europe and Canada in the 1980s for advanced prostate cancer and also used in endometriosis and fertility treatment; it is not sold in the United States.
Histrelin is a GnRH agonist delivered by a small implant under the skin of the arm that lasts a whole year, approved in the United States as Vantas for palliative treatment of advanced prostate cancer and as Supprelin for early puberty in children.
Query for this target: (TITLE:"GnRH receptor" OR ABSTRACT:"GnRH receptor" OR TITLE:"GNRHR" OR ABSTRACT:"GNRHR") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about GnRH receptor (GNRHR), not a curated reading list.
Shares Histrelin, Buserelin, Degarelix, Goserelin / leuprolide (ovarian function suppression).
Shares Histrelin, Degarelix, Goserelin / leuprolide (ovarian function suppression), Leuprolide (leuprorelin) and GnRH agonists.
Shares Buserelin, Degarelix, Goserelin / leuprolide (ovarian function suppression), Prostate cancer.
Shares Buserelin, Goserelin / leuprolide (ovarian function suppression), Leuprolide (leuprorelin) and GnRH agonists, Prostate cancer.
Shares Histrelin, Goserelin / leuprolide (ovarian function suppression), Prostate cancer.
Shares Verity Pharmaceuticals, Buserelin, Goserelin / leuprolide (ovarian function suppression), Leuprolide (leuprorelin) and GnRH agonists.
Shares Degarelix, Goserelin / leuprolide (ovarian function suppression), Leuprolide (leuprorelin) and GnRH agonists, Prostate cancer.