GnRH receptor (GNRHR)
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
G protein-coupled receptor on pituitary gonadotrophs; agonist-induced desensitisation or antagonist blockade suppresses LH and FSH release.
- 3 · How drugs use it
No product in this corpus aims at GnRH receptor (GNRHR) yet. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
External identifiers
Biology
G protein-coupled receptor on pituitary gonadotrophs; agonist-induced desensitisation or antagonist blockade suppresses LH and FSH release.
- Prostate cancer (androgen deprivation)
- Pre-menopausal hormone receptor-positive breast cancer (ovarian suppression)
Latest papers
topQuery 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.
Similar pages
not linked directly; found by shared links- TreatmentTriptorelin
Shares Goserelin / leuprolide (ovarian function suppression), Leuprolide (leuprorelin) and GnRH agonists, Prostate cancer, HR-positive / HER2-negative breast cancer.
- TermOvarian function suppression (OFS)
Shares Goserelin / leuprolide (ovarian function suppression), Leuprolide (leuprorelin) and GnRH agonists, HR-positive / HER2-negative breast cancer.
- TermAndrogen deprivation therapy (ADT)
Shares Degarelix, Leuprolide (leuprorelin) and GnRH agonists, Prostate cancer.
- TrialSOFT & TEXT
Shares Goserelin / leuprolide (ovarian function suppression), HR-positive / HER2-negative breast cancer.
- TermCastration-resistant prostate cancer (CRPC)
Shares Leuprolide (leuprorelin) and GnRH agonists, Prostate cancer.
- TechnologyAndrogen deprivation & AR pathway inhibitors
Shares Degarelix, Leuprolide (leuprorelin) and GnRH agonists, Prostate cancer.
- CancerMale breast cancer
Shares Goserelin / leuprolide (ovarian function suppression), HR-positive / HER2-negative breast cancer.
- TargetAndrogen receptor
Shares Degarelix, Leuprolide (leuprorelin) and GnRH agonists, Prostate cancer.