Glucocorticoid receptor (NR3C1)
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.
Overview
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.
- 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 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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
Ligand-activated nuclear receptor; in lymphoid cells its transcriptional programme induces apoptosis, the basis of steroid use in leukaemia, lymphoma and myeloma.
- 3 · How drugs use it
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.
External identifiers
Biology
Ligand-activated nuclear receptor; in lymphoid cells its transcriptional programme induces apoptosis, the basis of steroid use in leukaemia, lymphoma and myeloma.
- Acute lymphoblastic leukaemia
- Multiple myeloma
- Hodgkin and non-Hodgkin lymphoma
- Supportive care across cancers
Latest papers
topQuery 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.
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