{"entity":{"id":"gnrhr","kind":"target","name":"GnRH receptor (GNRHR)","aka":[],"tldr":"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.","summary":"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.","asOf":"2026-09-04","wikipedia":"https://en.wikipedia.org/wiki/Gonadotropin-releasing_hormone_receptor","links":[{"label":"UniProt P30968: GNRHR","url":"https://www.uniprot.org/uniprotkb/P30968/entry"}],"tags":[],"related":[],"cancers":["prostate","breast-hr-positive"],"sections":[],"technologies":[],"targets":[],"drugs":["leuprolide","goserelin","degarelix"],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"symbol":"GNRHR","role":[],"sources":[],"specificity":"tumour-associated","distribution":"few-types","specificityNote":"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.)","specificitySources":[{"label":"Human Protein Atlas GNRHR tissue","url":"https://www.proteinatlas.org/ENSG00000109163-GNRHR/tissue","note":"RNA tissue and blood lineage specificity, normal tissue antibody staining (version 25.1, CC BY-SA 3.0)"},{"label":"Human Protein Atlas GNRHR pathology","url":"https://www.proteinatlas.org/ENSG00000109163-GNRHR/pathology","note":"patients per staining level per cancer type (version 25.1, CC BY-SA 3.0)"},{"label":"Open Targets ENSG00000109163 associations","url":"https://platform.opentargets.org/target/ENSG00000109163/associations","note":"cancer associations at or above 0.5 (CC0)"}],"hgnc":"HGNC:4421","ensembl":"ENSG00000109163","uniprot":"P30968","entrez":"2798","firstDescribed":1992,"firstDescribedBasis":"sequence","firstDescribedNote":"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\".","firstDescribedSource":"https://pubmed.ncbi.nlm.nih.gov/1333190/","biology":"G protein-coupled receptor on pituitary gonadotrophs; agonist-induced desensitisation or antagonist blockade suppresses LH and FSH release.","whereFound":["Prostate cancer (androgen deprivation)","Pre-menopausal hormone receptor-positive breast cancer (ovarian suppression)"],"targetClass":"other","prevalence":[{"cancerId":"prostate","pct":"host","measure":"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."}]},"route":"/targets/gnrhr/","neighbours":{"cancer":[{"id":"breast-hr-positive","kind":"cancer","name":"HR-positive / HER2-negative breast cancer","route":"/cancers/breast-hr-positive/"},{"id":"prostate","kind":"cancer","name":"Prostate cancer","route":"/cancers/prostate/"}],"drug":[{"id":"abarelix","kind":"drug","name":"Abarelix","route":"/drugs/abarelix/"},{"id":"buserelin","kind":"drug","name":"Buserelin","route":"/drugs/buserelin/"},{"id":"degarelix","kind":"drug","name":"Degarelix","route":"/drugs/degarelix/"},{"id":"goserelin","kind":"drug","name":"Goserelin / leuprolide (ovarian function suppression)","route":"/drugs/goserelin/"},{"id":"histrelin","kind":"drug","name":"Histrelin","route":"/drugs/histrelin/"},{"id":"leuprolide","kind":"drug","name":"Leuprolide (leuprorelin) and GnRH agonists","route":"/drugs/leuprolide/"}],"company":[{"id":"tolmar","kind":"company","name":"Tolmar","route":"/companies/tolmar/"},{"id":"verity-pharma","kind":"company","name":"Verity Pharmaceuticals","route":"/companies/verity-pharma/"}]}}