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The receptor that steroid hormones switch on inside cells. In lymphoid cancers, dexamethasone and prednisone acting through it kill malignant lymphocytes directly, which is why steroids sit inside leukaemia, lymphoma and myeloma regimens as well as easing nausea and swelling.
The glucocorticoid receptor is a nuclear receptor that, once bound by cortisol or a synthetic steroid, moves into the nucleus and reprogrammes transcription. In lymphoblasts, plasma cells and lymphoma cells this programme is pro-apoptotic, so dexamethasone and prednisone are active anticancer drugs in acute lymphoblastic leukaemia, Hodgkin and non-Hodgkin lymphoma and multiple myeloma, and dexamethasone is the partner of almost every myeloma combination. Loss of receptor function is a mechanism of steroid resistance in relapsed leukaemia. Steroids also treat the swelling around brain tumours, immune-related side effects, and chemotherapy-induced nausea, and prevent the hypersensitivity reactions of taxanes.
In plain words · The receptor that steroid hormones switch on inside cells. In lymphoid cancers, dexamethasone and prednisone acting through it kill malignant lymphocytes directly, which is why steroids sit inside leukaemia, lymphoma and myeloma regimens as well as easing nausea and swelling.
The receptor that steroid hormones switch on inside cells. In lymphoid cancers, dexamethasone and prednisone acting through it kill malignant lymphocytes directly, which is why steroids sit inside leukaemia, lymphoma and myeloma regimens as well as easing nausea and swelling.
Ligand-activated nuclear receptor; in lymphoid cells its transcriptional programme induces apoptosis, the basis of steroid use in leukaemia, lymphoma and myeloma.
No product in this corpus aims at Glucocorticoid receptor (NR3C1) yet. Drugs cut off the hormone supply, block the receptor so the hormone cannot bind, or send the receptor to the cell's waste disposal.
Broadly expressed or essential: HPA finds the RNA at low tissue specificity; the 2 medicines aimed at it (Dexamethasone, Prednisone) act on the wild-type protein, so normal tissue is exposed and the therapeutic window comes from the tumour's faster division or its dependence on the protein. HPA NR3C1: RNA low tissue specificity; high antibody staining in 35 normal tissues; highest cancer staining renal cancer (10 of 12 high). Distribution: 3 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Leukaemia, Multiple myeloma, Lymphoma); Open Targets associates it with 5 specific cancer types at or above 0.5 (plasma cell myeloma, prostate cancer, lymphoma, leukemia, mycosis fungoides). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas NR3C1 tissue; Open Targets ENSG00000113580 associations
First described 1985. Earliest sequence paper UniProt cites for the protein: Hollenberg S.M. et al, Nature, 1985, "Primary structure and expression of a functional human glucocorticoid receptor cDNA". Source.
Ligand-activated nuclear receptor; in lymphoid cells its transcriptional programme induces apoptosis, the basis of steroid use in leukaemia, lymphoma and myeloma.
RNA: low tissue specificity, detected in all normal tissues.
Medium: Adrenal gland, Cerebellum, Colon, Endometrium, Heart muscle, Hippocampus, Rectum, Small intestine.
Medium only: colorectal cancer, endometrial cancer, stomach cancer, testis cancer.
HPA NR3C1 tissue · HPA NR3C1 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 |
|---|---|---|---|---|
| Acute lymphoblastic leukaemia | nearly all% | Glucocorticoid receptor expressed in lymphoblasts; prednisone response is a prognostic marker | cancer.gov |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query for this target: (TITLE:"Glucocorticoid receptor" OR ABSTRACT:"Glucocorticoid receptor" OR TITLE:"NR3C1" OR ABSTRACT:"NR3C1") 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 Glucocorticoid receptor (NR3C1), not a curated reading list.
Shares Dexamethasone, Multiple myeloma.
Shares Dexamethasone, Hodgkin lymphoma, Multiple myeloma.
Shares Dexamethasone, Multiple myeloma.
Shares Prednisone, Diffuse large B-cell lymphoma.
Shares Prednisone, Dexamethasone, Acute lymphoblastic leukaemia.
Shares Dexamethasone, Multiple myeloma.
Shares Dexamethasone, Multiple myeloma.
Shares Dexamethasone, Multiple myeloma.