Loading
The retinoid X receptor is a switch inside cells that vitamin A-like molecules turn on to change which genes are active; bexarotene uses it to make lymphoma cells in the skin mature and die.
RXR alpha, beta and gamma are nuclear receptors that form heterodimers with retinoic acid receptors, the vitamin D receptor, thyroid hormone receptor, PPARs and LXR, so a single RXR ligand can alter several transcriptional programmes at once. Bexarotene, a selective RXR agonist (rexinoid), is approved for cutaneous T-cell lymphoma; its metabolic side effects (central hypothyroidism, hypertriglyceridaemia) follow directly from RXR partner activation. The related retinoic acid receptor is the target of all-trans retinoic acid in acute promyelocytic leukaemia.
In plain words · The retinoid X receptor is a switch inside cells that vitamin A-like molecules turn on to change which genes are active; bexarotene uses it to make lymphoma cells in the skin mature and die.
The retinoid X receptor is a switch inside cells that vitamin A-like molecules turn on to change which genes are active; bexarotene uses it to make lymphoma cells in the skin mature and die.
Ligand binding recruits co-activators and drives differentiation and apoptosis genes in malignant T cells; RXR also modulates PPAR-gamma-dependent lipid metabolism.
3 products aim at Retinoid X receptor (RXR): small molecules. 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 3 medicines aimed at it (Acitretin, Bexarotene, Isotretinoin) 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 RXRA: RNA low tissue specificity; blood lineage group enriched (granulocytes 20 nTPM, monocytes 13 nTPM); high antibody staining in 32 normal tissues; highest cancer staining lung cancer (12 of 12 high). HPA RXRB: RNA low tissue specificity; high antibody staining in 32 normal tissues; highest cancer staining breast cancer (11 of 11 high). HPA RXRG: RNA tissue enhanced (pituitary gland 30 nTPM, retina 23 nTPM, skeletal muscle 47 nTPM); no normal tissue stained high; highest cancer staining carcinoid (1 of 4 high). Distribution: no corpus cancer carries a prevalence row, threshold or catalogue link for it; Open Targets associates it with 2 specific cancer types at or above 0.5 (primary cutaneous T-cell non-Hodgkin lymphoma, urinary bladder cancer). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas RXRA tissue; Human Protein Atlas RXRB tissue; Human Protein Atlas RXRG tissue; Open Targets ENSG00000186350 associations; Open Targets ENSG00000204231 associations
Ligand binding recruits co-activators and drives differentiation and apoptosis genes in malignant T cells; RXR also modulates PPAR-gamma-dependent lipid metabolism.
RNA: low tissue specificity, detected in all normal tissues. Blood: group enriched (granulocytes 20 nTPM, monocytes 13 nTPM).
Medium: Adipose tissue, Cerebral cortex, Duodenum, Epididymis, Gallbladder, Hippocampus, Kidney, Liver.
Medium only: head and neck cancer.
HPA RXRA tissue · HPA RXRA pathology · HPA protein class: FDA approved drug targets
RNA: low tissue specificity, detected in many normal tissues.
Medium: Adipose tissue, Breast, Hippocampus, Liver, Prostate, Salivary gland, Small intestine, Smooth muscle.
HPA RXRB tissue · HPA RXRB pathology · HPA protein class: FDA approved drug targets
RNA: tissue enhanced (pituitary gland 30 nTPM, retina 23 nTPM, skeletal muscle 47 nTPM), detected in many normal tissues.
No normal tissue stained high.
RNA group enriched: Skin Cutaneous Melanoma 56 pTPM, Thyroid Carcinoma 68 pTPM.
Medium only: breast cancer, colorectal cancer, glioma, head and neck cancer.
HPA RXRG tissue · HPA RXRG 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 |
|---|---|---|---|---|
| Metastatic cancer | all% | Signalling protein present in most cells (retinoid X receptor); bexarotene acts on the pathway rather than on a mutation that selects patients, so no prevalence applies. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Acitretin is a vitamin A tablet licensed for severe psoriasis. In people who have had an organ transplant and keep developing skin cancers, it reduces the number of new squamous cell carcinomas while it is taken.
Bexarotene (Targretin) is a vitamin A-like capsule and gel for the skin disease of cutaneous T-cell lymphoma when other treatments have stopped working.
Isotretinoin, the acne drug, is given to children with high-risk neuroblastoma for six months after transplant to nudge any surviving cancer cells into growing up into harmless nerve cells. A 1999 trial showed it improved survival and it has been part of standard care since.
Query for this target: (TITLE:"Retinoid X receptor" OR ABSTRACT:"Retinoid X receptor" OR TITLE:"RXR" OR ABSTRACT:"RXR" OR TITLE:"RXRA" OR ABSTRACT:"RXRA" OR TITLE:"RXRB" OR ABSTRACT:"RXRB" OR TITLE:"RXRG" OR ABSTRACT:"RXRG") 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 Retinoid X receptor (RXR), not a curated reading list.
Shares Acitretin, Isotretinoin.
Shares Acute myeloid leukaemia (KEGG map), Small cell lung cancer (KEGG map).