RXRB
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Also known as NR2B2H-2RIIBPRCoR-1RXRbetaRXR-beta
Summary
RXRB (retinoid X receptor beta, HGNC:10478) is a protein-coding gene on chromosome 6p21.32, encoding Retinoic acid receptor RXR-beta (P28702). Receptor for retinoic acid.
This gene encodes a member of the retinoid X receptor (RXR) family of nuclear receptors which are involved in mediating the effects of retinoic acid (RA). The encoded protein forms homodimers with the retinoic acid, thyroid hormone, and vitamin D receptors, increasing both DNA binding and transcriptional function on their respective response elements. This gene lies within the major histocompatibility complex (MHC) class II region on chromosome 6. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene.
Source: NCBI Gene 6257 — RefSeq curated summary.
At a glance
- GWAS associations: 1
- Clinical variants (ClinVar): 69 total
- Druggable target: yes — 6 molecules with ChEMBL bioactivity
- Transcription factor: yes — 19 downstream targets (CollecTRI)
- MANE Select transcript:
NM_021976
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:10478 |
| Approved symbol | RXRB |
| Name | retinoid X receptor beta |
| Location | 6p21.32 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | NR2B2, H-2RIIBP, RCoR-1, RXRbeta, RXR-beta |
| Ensembl gene | ENSG00000204231 |
| Ensembl biotype | protein_coding |
| OMIM | 180246 |
| Entrez | 6257 |
Gene structure
Transcript identifiers
Ensembl transcripts: 13 — 10 protein_coding, 2 retained_intron, 1 nonsense_mediated_decay
ENST00000374680, ENST00000374685, ENST00000481441, ENST00000483281, ENST00000483821, ENST00000865272, ENST00000865273, ENST00000865274, ENST00000865275, ENST00000865276, ENST00000865277, ENST00000865278, ENST00000912952
RefSeq mRNA: 3 — MANE Select: NM_021976
NM_001270401, NM_001291989, NM_021976
CCDS: CCDS4768, CCDS59007
Canonical transcript exons
ENST00000374680 — 10 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001726956 | 33199169 | 33199416 |
| ENSE00001854541 | 33200242 | 33200665 |
| ENSE00001946150 | 33193588 | 33194829 |
| ENSE00003458331 | 33195570 | 33195702 |
| ENSE00003490395 | 33194945 | 33195050 |
| ENSE00003513613 | 33195363 | 33195454 |
| ENSE00003568955 | 33197762 | 33197941 |
| ENSE00003580725 | 33196434 | 33196606 |
| ENSE00003629815 | 33198308 | 33198464 |
| ENSE00003644074 | 33195907 | 33196036 |
Expression profiles
Bgee: expression breadth ubiquitous, 134 present calls, max score 96.26.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 28.4122 / max 143.4359, expressed in 1813 samples.
FANTOM5 promoters (4 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 73105 | 19.6379 | 1798 |
| 73104 | 8.5437 | 1751 |
| 73103 | 0.1937 | 109 |
| 73102 | 0.0369 | 17 |
Top tissues by expression
134 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right lobe of thyroid gland | UBERON:0001119 | 96.26 | gold quality |
| granulocyte | CL:0000094 | 96.06 | gold quality |
| mucosa of stomach | UBERON:0001199 | 96.05 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 96.03 | gold quality |
| right coronary artery | UBERON:0001625 | 95.92 | gold quality |
| right uterine tube | UBERON:0001302 | 95.75 | gold quality |
| body of uterus | UBERON:0009853 | 95.72 | gold quality |
| thyroid gland | UBERON:0002046 | 95.71 | gold quality |
| right ovary | UBERON:0002118 | 95.59 | gold quality |
| pituitary gland | UBERON:0000007 | 95.58 | gold quality |
| endocervix | UBERON:0000458 | 95.57 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 95.50 | gold quality |
| apex of heart | UBERON:0002098 | 95.35 | gold quality |
| tibial nerve | UBERON:0001323 | 95.34 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 95.30 | gold quality |
| spleen | UBERON:0002106 | 95.28 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 95.25 | gold quality |
| adenohypophysis | UBERON:0002196 | 95.20 | gold quality |
| left ovary | UBERON:0002119 | 95.18 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 95.13 | gold quality |
| lower esophagus | UBERON:0013473 | 95.12 | gold quality |
| left uterine tube | UBERON:0001303 | 95.07 | gold quality |
| cerebellum | UBERON:0002037 | 95.00 | gold quality |
| cerebellar cortex | UBERON:0002129 | 95.00 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 95.00 | gold quality |
| tibial artery | UBERON:0007610 | 94.96 | gold quality |
| popliteal artery | UBERON:0002250 | 94.94 | gold quality |
| fundus of stomach | UBERON:0001160 | 94.93 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 94.88 | gold quality |
| ascending aorta | UBERON:0001496 | 94.86 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 2.35 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
19 targets.
| Target | Regulation |
|---|---|
| ABCG1 | |
| ALDH1A1 | Activation |
| CD74 | |
| CRYAB | |
| CTNNB1 | |
| GH1 | |
| GPRC5A | |
| ICAM1 | Unknown |
| IFNG | Activation |
| LRP1 | |
| PCP2 | |
| PKD1 | Activation |
| PTH | Repression |
| RARB | Activation |
| RBP1 | Repression |
| RBP2 | Unknown |
| SUPT7L | |
| TRH | |
| TSHB |
JASPAR motifs
| Motif | Name | Family |
|---|---|---|
| MA0855.1 | RXRB | RXR-related receptors (NR2) |
| MA1555.1 | RXRB | RXR-related receptors (NR2) |
JASPAR matrix evidence (PMIDs): PMID:15019979, PMID:14559106
Upstream regulators (CollecTRI, top): THRA
miRNA regulators (miRDB)
57 targeting RXRB, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-4747-5P | 100.00 | 67.90 | 2681 |
| HSA-MIR-5196-5P | 100.00 | 67.98 | 2761 |
| HSA-MIR-3689D | 100.00 | 66.14 | 1181 |
| HSA-MIR-6851-5P | 100.00 | 65.63 | 1294 |
| HSA-MIR-513A-5P | 100.00 | 69.77 | 2465 |
| HSA-MIR-6077 | 99.99 | 68.04 | 2299 |
| HSA-MIR-101-3P | 99.94 | 75.03 | 2230 |
| HSA-MIR-3682-5P | 99.93 | 67.97 | 1163 |
| HSA-MIR-4731-5P | 99.89 | 67.23 | 2537 |
| HSA-MIR-9902 | 99.89 | 69.15 | 2250 |
| HSA-MIR-4492 | 99.87 | 68.25 | 3611 |
| HSA-MIR-765 | 99.84 | 68.24 | 2442 |
| HSA-MIR-6739-5P | 99.80 | 67.87 | 2806 |
| HSA-MIR-11181-3P | 99.75 | 66.38 | 2205 |
| HSA-MIR-6733-5P | 99.74 | 67.94 | 2759 |
| HSA-MIR-12124 | 99.68 | 69.17 | 2700 |
| HSA-MIR-6887-3P | 99.66 | 67.83 | 1778 |
| HSA-MIR-298 | 99.63 | 67.56 | 1916 |
| HSA-MIR-6132 | 99.60 | 65.83 | 1554 |
| HSA-MIR-6836-5P | 99.60 | 65.62 | 1538 |
| HSA-MIR-3153 | 99.55 | 67.59 | 2337 |
| HSA-MIR-4753-5P | 99.54 | 68.51 | 1356 |
| HSA-MIR-6828-5P | 99.31 | 69.21 | 1433 |
| HSA-MIR-4685-5P | 99.25 | 65.99 | 1563 |
| HSA-MIR-6837-5P | 99.25 | 65.47 | 1632 |
| HSA-MIR-1253 | 99.12 | 67.08 | 1688 |
| HSA-MIR-7854-3P | 99.08 | 66.26 | 1117 |
| HSA-MIR-622 | 98.99 | 66.48 | 1050 |
| HSA-MIR-6770-5P | 98.97 | 66.76 | 1853 |
| HSA-MIR-3922-5P | 98.77 | 66.53 | 1059 |
Literature-anchored findings (GeneRIF, showing 13)
- The role of retinoid X receptor messenger RNA expression in curatively resected non-small cell lung cancer (PMID:11839661)
- polymorphism is unrelated to schizophrenia or alcoholism. (PMID:11840500)
- Family studies revealed significant linkage disequilibrium between the RXRB alleles and a number of HLA-DPB1 alleles. (PMID:12175732)
- Diminished RXRbeta expression might be related to prostate cancer progression. Because responsiveness to retinoic acid treatments depends on expression of different receptors, it is important to study their expression before therapy. (PMID:12514092)
- partial dissociation of TR/retinoid X receptor heterodimer complex from the TRE is involved in the suppression of transcription induced by polychlorinated biphenyls (PMID:14985366)
- The retinoid X receptor, beta is expressed widely and can be found in almost every tissue. (PMID:15608692)
- In the RXRB polymorphism, no genotype TT is observed in patients with psoriasis guttata with a positive personal history of repeated tonsillitis (p(corr) = 0.001). (PMID:17341859)
- In healthy elderly men reduction of RXRbeta expression in peripheral blood mononuclear cells might be a common feature of physiological senescence. (PMID:17916375)
- PPARgamma/retinoid X receptor complex released from activated platelets in microparticles was internalized by a monocytic cell line. (PMID:18217139)
- A fatty acid-binding protein 7/RXRbeta pathway enhances survival and proliferation in triple-negative breast cancer. (PMID:22322885)
- RXR interaction is necessary for NPM-RAR-mediated myeloid maturation arrest. (PMID:24183235)
- Data show that pregnane X receptor/retinoid X receptor PXR/RXR-[alpha], RXR-[beta], or RXR-[gamma] expression was noted in 9 (16.4%), 9 (16.4%), and 10 (18.2%) pancreatic adenocarcinoma cases, respectively. (PMID:26355550)
- Genetic variant of RXR involved in the vitamin D metabolic pathway was linked to HCV infection outcomes among a high-risk Chinese population. (PMID:33246082)
Cross-species orthologs
31 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | rxrbb | ENSDARG00000002006 |
| danio_rerio | rxrba | ENSDARG00000078954 |
| mus_musculus | Rxrb | ENSMUSG00000039656 |
| rattus_norvegicus | Rxrb | ENSRNOG00000000464 |
| drosophila_melanogaster | usp | FBGN0003964 |
| drosophila_melanogaster | Hr78 | FBGN0015239 |
| drosophila_melanogaster | Hr83 | FBGN0037436 |
| caenorhabditis_elegans | WBGENE00003626 | |
| caenorhabditis_elegans | WBGENE00003650 | |
| caenorhabditis_elegans | nhr-69 | WBGENE00003659 |
| caenorhabditis_elegans | WBGENE00003683 | |
| caenorhabditis_elegans | WBGENE00003706 | |
| caenorhabditis_elegans | WBGENE00003719 | |
| caenorhabditis_elegans | WBGENE00003726 | |
| caenorhabditis_elegans | WBGENE00007547 | |
| caenorhabditis_elegans | WBGENE00008221 | |
| caenorhabditis_elegans | WBGENE00011097 | |
| caenorhabditis_elegans | WBGENE00011098 | |
| caenorhabditis_elegans | WBGENE00011099 | |
| caenorhabditis_elegans | WBGENE00011100 | |
| caenorhabditis_elegans | WBGENE00015395 | |
| caenorhabditis_elegans | WBGENE00015396 | |
| caenorhabditis_elegans | WBGENE00015397 | |
| caenorhabditis_elegans | WBGENE00015705 | |
| caenorhabditis_elegans | WBGENE00016975 | |
| caenorhabditis_elegans | WBGENE00017198 | |
| caenorhabditis_elegans | WBGENE00017787 | |
| caenorhabditis_elegans | WBGENE00020748 | |
| caenorhabditis_elegans | WBGENE00021848 | |
| caenorhabditis_elegans | WBGENE00022423 | |
| caenorhabditis_elegans | WBGENE00044354 |
Paralogs (11): HNF4A (ENSG00000101076), NR2E1 (ENSG00000112333), NR2C1 (ENSG00000120798), RXRG (ENSG00000143171), NR2F6 (ENSG00000160113), HNF4G (ENSG00000164749), NR2F1 (ENSG00000175745), NR2C2 (ENSG00000177463), NR2F2 (ENSG00000185551), RXRA (ENSG00000186350), NR2E3 (ENSG00000278570)
Protein
Protein identifiers
Retinoic acid receptor RXR-beta — P28702 (reviewed: P28702)
Alternative names: Nuclear receptor subfamily 2 group B member 2, Retinoid X receptor beta
All UniProt accessions (5): A0A0S2Z4M5, A0A0S2Z570, E9PK75, P28702, Q5STP9
UniProt curated annotations — full annotation on UniProt →
Function. Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE).
Subunit / interactions. Homodimer (in vitro). Heterodimer with other retinoic acid receptor family members. Binds DNA preferentially as a RAR/RXR heterodimer. Interacts with NR1H3. Interacts with AKAP13.
Subcellular location. Nucleus. Cytoplasm.
Tissue specificity. Expressed in aortic endothelial cells (at protein level). Expressed in monocytes. Expressed in a variety of tumor cell lines.
Domain organisation. Composed of three domains: a modulating N-terminal domain, a DNA-binding domain and a C-terminal ligand-binding domain.
Induction. Down-regulated by aging.
Similarity. Belongs to the nuclear hormone receptor family. NR2 subfamily.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P28702-1 | 1 | yes |
| P28702-3 | 2 |
RefSeq proteins (3): NP_001257330, NP_001278918, NP_068811* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000003 | Retinoid-X_rcpt/HNF4 | Family |
| IPR000536 | Nucl_hrmn_rcpt_lig-bd | Domain |
| IPR001628 | Znf_hrmn_rcpt | Domain |
| IPR001723 | Nuclear_hrmn_rcpt | Family |
| IPR013088 | Znf_NHR/GATA | Homologous_superfamily |
| IPR035500 | NHR-like_dom_sf | Homologous_superfamily |
| IPR050274 | Nuclear_hormone_rcpt_NR2 | Family |
Pfam: PF00104, PF00105
UniProt features (37 total): helix 12, compositionally biased region 8, region of interest 6, strand 2, zinc finger region 2, chain 1, domain 1, modified residue 1, DNA-binding region 1, splice variant 1, sequence conflict 1, turn 1
Structure
Experimental structures (PDB)
7 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7A78 | X-RAY DIFFRACTION | 1.72 |
| 5KYA | X-RAY DIFFRACTION | 2.6 |
| 5HJP | X-RAY DIFFRACTION | 2.6 |
| 5I4V | X-RAY DIFFRACTION | 2.61 |
| 1H9U | X-RAY DIFFRACTION | 2.7 |
| 5KYJ | X-RAY DIFFRACTION | 2.8 |
| 1UHL | X-RAY DIFFRACTION | 2.9 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P28702-F1 | 72.81 | 0.49 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Post-translational modifications (1): 25
Function
Pathways and Gene Ontology
Reactome pathways
18 pathways
| ID | Pathway |
|---|---|
| R-HSA-1989781 | PPARA activates gene expression |
| R-HSA-383280 | Nuclear Receptor transcription pathway |
| R-HSA-5362517 | Signaling by Retinoic Acid |
| R-HSA-9029558 | NR1H2 & NR1H3 regulate gene expression linked to lipogenesis |
| R-HSA-9029569 | NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux |
| R-HSA-9031525 | NR1H2 & NR1H3 regulate gene expression to limit cholesterol uptake |
| R-HSA-9031528 | NR1H2 & NR1H3 regulate gene expression linked to triglyceride lipolysis in adipose |
| R-HSA-9623433 | NR1H2 & NR1H3 regulate gene expression to control bile acid homeostasis |
| R-HSA-9632974 | NR1H2 & NR1H3 regulate gene expression linked to gluconeogenesis |
| R-HSA-1430728 | Metabolism |
| R-HSA-162582 | Signal Transduction |
| R-HSA-212436 | Generic Transcription Pathway |
| R-HSA-400206 | Regulation of lipid metabolism by PPARalpha |
| R-HSA-556833 | Metabolism of lipids |
| R-HSA-73857 | RNA Polymerase II Transcription |
| R-HSA-74160 | Gene expression (Transcription) |
| R-HSA-9006931 | Signaling by Nuclear Receptors |
| R-HSA-9024446 | NR1H2 and NR1H3-mediated signaling |
MSigDB gene sets: 258 (showing top):
GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_MUSCLE_TISSUE_DEVELOPMENT, KEGG_ADIPOCYTOKINE_SIGNALING_PATHWAY, MACLACHLAN_BRCA1_TARGETS_DN, GOBP_CELLULAR_RESPONSE_TO_LIPID, MORF_SNRP70, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, GOBP_GROWTH, GOBP_STRIATED_MUSCLE_CELL_DIFFERENTIATION, GOBP_VENTRICULAR_CARDIAC_MUSCLE_CELL_DIFFERENTIATION, GOBP_MUSCLE_CELL_PROLIFERATION, BROWNE_HCMV_INFECTION_12HR_UP, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, USF_C
GO Biological Process (16): in utero embryonic development (GO:0001701), maternal placenta development (GO:0001893), nervous system development (GO:0007399), hormone-mediated signaling pathway (GO:0009755), cell differentiation (GO:0030154), positive regulation of bone mineralization (GO:0030501), mRNA transcription by RNA polymerase II (GO:0042789), positive regulation of DNA-templated transcription (GO:0045893), positive regulation of transcription by RNA polymerase II (GO:0045944), retinoic acid receptor signaling pathway (GO:0048384), ventricular cardiac muscle cell differentiation (GO:0055012), cardiac muscle cell proliferation (GO:0060038), positive regulation of vitamin D receptor signaling pathway (GO:0070564), cellular response to retinoic acid (GO:0071300), regulation of DNA-templated transcription (GO:0006355), nuclear receptor-mediated steroid hormone signaling pathway (GO:0030518)
GO Molecular Function (15): RNA polymerase II transcription regulatory region sequence-specific DNA binding (GO:0000977), DNA-binding transcription factor activity, RNA polymerase II-specific (GO:0000981), DNA-binding transcription activator activity, RNA polymerase II-specific (GO:0001228), nuclear steroid receptor activity (GO:0003707), nuclear receptor activity (GO:0004879), zinc ion binding (GO:0008270), chromatin DNA binding (GO:0031490), retinoic acid-responsive element binding (GO:0044323), sequence-specific double-stranded DNA binding (GO:1990837), transcription cis-regulatory region binding (GO:0000976), DNA binding (GO:0003677), DNA-binding transcription factor activity (GO:0003700), protein binding (GO:0005515), sequence-specific DNA binding (GO:0043565), metal ion binding (GO:0046872)
GO Cellular Component (7): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730), cytosol (GO:0005829), RNA polymerase II transcription regulator complex (GO:0090575), cytoplasm (GO:0005737)
Reactome top-level categories
Rollup of top-9 pathways:
| Category | Pathways |
|---|---|
| NR1H2 and NR1H3-mediated signaling | 6 |
| Signaling by Nuclear Receptors | 2 |
| Regulation of lipid metabolism by PPARalpha | 1 |
| Generic Transcription Pathway | 1 |
| RNA Polymerase II Transcription | 1 |
| Metabolism of lipids | 1 |
| Metabolism | 1 |
| Gene expression (Transcription) | 1 |
| Signal Transduction | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 4 |
| transcription by RNA polymerase II | 2 |
| DNA-templated transcription | 2 |
| regulation of DNA-templated transcription | 2 |
| regulation of transcription by RNA polymerase II | 2 |
| nuclear receptor-mediated signaling pathway | 2 |
| transcription cis-regulatory region binding | 2 |
| RNA polymerase II transcription regulatory region sequence-specific DNA binding | 2 |
| DNA-binding transcription factor activity, RNA polymerase II-specific | 2 |
| DNA binding | 2 |
| nuclear lumen | 2 |
| chordate embryonic development | 1 |
| placenta development | 1 |
| developmental process involved in reproduction | 1 |
| anatomical structure development | 1 |
| maternal process involved in female pregnancy | 1 |
| system development | 1 |
| signal transduction | 1 |
| cellular response to hormone stimulus | 1 |
| cellular developmental process | 1 |
| bone mineralization | 1 |
| regulation of bone mineralization | 1 |
| positive regulation of ossification | 1 |
| positive regulation of biomineral tissue development | 1 |
| mRNA transcription | 1 |
| positive regulation of RNA biosynthetic process | 1 |
| positive regulation of DNA-templated transcription | 1 |
| hormone-mediated signaling pathway | 1 |
| cardiac muscle cell differentiation | 1 |
| striated muscle cell proliferation | 1 |
| cardiac muscle tissue growth | 1 |
| vitamin D receptor signaling pathway | 1 |
| regulation of vitamin D receptor signaling pathway | 1 |
| positive regulation of intracellular signal transduction | 1 |
| response to retinoic acid | 1 |
| cellular response to lipid | 1 |
| cellular response to oxygen-containing compound | 1 |
| regulation of gene expression | 1 |
| regulation of RNA biosynthetic process | 1 |
| steroid hormone receptor signaling pathway | 1 |
Protein interactions and networks
STRING
1094 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| RXRB | COL11A2 | P13942 | 804 |
| RXRB | SLC39A7 | Q92504 | 797 |
| RXRB | HSD17B8 | Q92506 | 795 |
| RXRB | RGL2 | O15211 | 770 |
| RXRB | RARS1 | P54136 | 761 |
| RXRB | RARA | P10276 | 757 |
| RXRB | RARB | P10826 | 755 |
| RXRB | KIFC1 | Q9BW19 | 745 |
| RXRB | RPS18 | P25232 | 735 |
| RXRB | CNOT7 | Q9UIV1 | 671 |
| RXRB | RING1 | Q06587 | 665 |
| RXRB | PFDN6 | O15212 | 665 |
| RXRB | PPARD | Q03181 | 595 |
| RXRB | NCOR1 | O75376 | 584 |
| RXRB | PPARA | Q07869 | 545 |
IntAct
122 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| RXRB | RARA | psi-mi:“MI:0915”(physical association) | 0.950 |
| RARA | RXRB | psi-mi:“MI:0915”(physical association) | 0.950 |
| RARB | RXRB | psi-mi:“MI:0915”(physical association) | 0.810 |
| RXRB | RARB | psi-mi:“MI:0915”(physical association) | 0.810 |
| RARA | NCOR1 | psi-mi:“MI:0914”(association) | 0.800 |
| RXRB | NR1H4 | psi-mi:“MI:0915”(physical association) | 0.790 |
| NR1H4 | RXRB | psi-mi:“MI:0915”(physical association) | 0.790 |
| RARG | RXRB | psi-mi:“MI:0915”(physical association) | 0.740 |
| RXRB | NR1H3 | psi-mi:“MI:0915”(physical association) | 0.720 |
BioGRID (97): RXRB (Two-hybrid), NR1H3 (Two-hybrid), RXRB (Affinity Capture-Western), RXRB (Affinity Capture-Western), RXRB (Affinity Capture-Western), RXRB (Affinity Capture-MS), RXRB (Two-hybrid), SPOP (Two-hybrid), NCOA1 (Two-hybrid), ADRBK1 (Affinity Capture-MS), CCNK (Affinity Capture-MS), CDC42BPB (Affinity Capture-MS), C2CD5 (Affinity Capture-MS), POLR3F (Affinity Capture-MS), AFF4 (Affinity Capture-MS)
ESM2 similar proteins: A0A0G2JUG7, A1YER5, A1YFY1, A2T6X5, B2DD29, C0HBT3, O08629, O15156, O15169, O35730, O60307, O95343, P0C0T2, P28702, P28704, P29353, P50241, P98083, Q06587, Q0IHB0, Q13263, Q2V2M9, Q2YDU3, Q3U1V8, Q3U2S4, Q4KMP7, Q5DU25, Q5JU85, Q5PRF9, Q5R7W7, Q5RBI7, Q5RJI5, Q5TJF3, Q5TJF7, Q62233, Q62318, Q66J69, Q68DC2, Q6MGB6, Q6ZRS2
Diamond homologs: A2T928, A2T929, A4IIG7, O35507, O42295, O42450, O57606, O77245, O97716, P03373, P04625, P10276, P10826, P10827, P10828, P11416, P12813, P13631, P15204, P17671, P18113, P18115, P18117, P18119, P18514, P18515, P18516, P18911, P19793, P22448, P22605, P22736, P22829, P28699, P28700, P28701, P28702, P28704, P28705, P37242
SIGNOR signaling
24 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| RXRB | up-regulates | PPARA | binding |
| RXRB | up-regulates | PPARD | binding |
| RXRB | up-regulates | PPARG | binding |
| RXRB | up-regulates | NR1H2 | binding |
| RARB | up-regulates | RXRB | binding |
| RARG | up-regulates | RXRB | binding |
| RXRB | up-regulates | RARA | binding |
| RXRB | up-regulates | RARB | binding |
| RXRB | “up-regulates quantity by expression” | RARB | “transcriptional regulation” |
| RXRB | up-regulates | RARG | binding |
| “all-trans-retinoic acid” | “up-regulates activity” | RXRB | “chemical activation” |
| bexarotene | “up-regulates activity” | RXRB | “chemical activation” |
| “9-cis-retinoic acid” | “up-regulates activity” | RXRB | “chemical activation” |
| RXRB | “up-regulates activity” | THR | binding |
| RXRB | up-regulates | RAR | binding |
| RXRB | up-regulates | THR | binding |
| RXRB | up-regulates | NR4A2 | binding |
| RXRB | up-regulates | NR2F1 | binding |
| RXRB | up-regulates | NR2F2 | binding |
| RXRB | up-regulates | THRA | binding |
| RXRB | up-regulates | THRB | binding |
| RXRB | up-regulates | NRIP1 | binding |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 50 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| SUMOylation of intracellular receptors | 9 | 75.6× | 2e-13 |
| Nuclear Receptor transcription pathway | 12 | 60.1× | 1e-16 |
| PPARA activates gene expression | 6 | 14.2× | 2e-04 |
| Activation of anterior HOX genes in hindbrain development during early embryogenesis | 5 | 11.4× | 2e-03 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| intracellular receptor signaling pathway | 5 | 103.3× | 3e-07 |
| retinoic acid receptor signaling pathway | 7 | 94.5× | 3e-10 |
| mRNA transcription by RNA polymerase II | 6 | 41.3× | 1e-06 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
69 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 48 |
| Likely benign | 10 |
| Benign | 4 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1289 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 6:33194827:AACC:A | acceptor_loss | 1.0000 |
| 6:33194829:CCT:C | acceptor_loss | 1.0000 |
| 6:33194940:CTCAC:C | donor_loss | 1.0000 |
| 6:33194941:TCA:T | donor_loss | 1.0000 |
| 6:33194942:CACCG:C | donor_loss | 1.0000 |
| 6:33194943:A:T | donor_loss | 1.0000 |
| 6:33194944:C:CG | donor_loss | 1.0000 |
| 6:33194944:CCGT:C | donor_gain | 1.0000 |
| 6:33194947:T:TA | donor_gain | 1.0000 |
| 6:33194948:C:A | donor_gain | 1.0000 |
| 6:33194964:A:AC | donor_gain | 1.0000 |
| 6:33194965:C:CC | donor_gain | 1.0000 |
| 6:33194965:CTT:C | donor_gain | 1.0000 |
| 6:33194967:T:TA | donor_gain | 1.0000 |
| 6:33195049:ATCTG:A | acceptor_loss | 1.0000 |
| 6:33195050:TCTGG:T | acceptor_loss | 1.0000 |
| 6:33195051:C:CC | acceptor_gain | 1.0000 |
| 6:33195051:CTGGG:C | acceptor_loss | 1.0000 |
| 6:33195056:A:AC | acceptor_gain | 1.0000 |
| 6:33195060:C:CT | acceptor_gain | 1.0000 |
| 6:33195061:A:T | acceptor_gain | 1.0000 |
| 6:33195568:A:AC | donor_gain | 1.0000 |
| 6:33195569:C:CC | donor_gain | 1.0000 |
| 6:33195588:A:AC | donor_gain | 1.0000 |
| 6:33195589:C:CC | donor_gain | 1.0000 |
| 6:33196032:TTTGG:T | acceptor_gain | 1.0000 |
| 6:33196470:AACGC:A | donor_gain | 1.0000 |
| 6:33196474:C:CA | donor_gain | 1.0000 |
| 6:33197756:CCTTA:C | donor_loss | 1.0000 |
| 6:33197757:CTTA:C | donor_loss | 1.0000 |
AlphaMissense
3418 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 6:33194707:A:G | L526P | 1.000 |
| 6:33194707:A:T | L526H | 1.000 |
| 6:33194719:A:C | L522R | 1.000 |
| 6:33194719:A:G | L522P | 1.000 |
| 6:33194719:A:T | L522H | 1.000 |
| 6:33194721:G:C | F521L | 1.000 |
| 6:33194721:G:T | F521L | 1.000 |
| 6:33194722:A:C | F521C | 1.000 |
| 6:33194722:A:G | F521S | 1.000 |
| 6:33194723:A:G | F521L | 1.000 |
| 6:33194728:T:A | D519V | 1.000 |
| 6:33194731:A:T | I518N | 1.000 |
| 6:33194743:C:A | G514V | 1.000 |
| 6:33194743:C:T | G514D | 1.000 |
| 6:33194746:A:T | I513N | 1.000 |
| 6:33194749:A:G | L512P | 1.000 |
| 6:33194749:A:T | L512H | 1.000 |
| 6:33194754:G:C | F510L | 1.000 |
| 6:33194754:G:T | F510L | 1.000 |
| 6:33194755:A:G | F510S | 1.000 |
| 6:33194756:A:G | F510L | 1.000 |
| 6:33194757:G:C | F509L | 1.000 |
| 6:33194757:G:T | F509L | 1.000 |
| 6:33194759:A:G | F509L | 1.000 |
| 6:33194760:A:C | F508L | 1.000 |
| 6:33194760:A:T | F508L | 1.000 |
| 6:33194761:A:C | F508C | 1.000 |
| 6:33194761:A:G | F508S | 1.000 |
| 6:33194762:A:G | F508L | 1.000 |
| 6:33194762:A:T | F508I | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000491541 (6:33194538 G>C,T), RS1000612226 (6:33194223 A>G), RS1001539000 (6:33195886 A>G), RS1001951266 (6:33201835 C>G), RS1002841616 (6:33200610 T>C), RS1002954205 (6:33200336 C>T), RS1003135587 (6:33194110 C>T), RS1003618541 (6:33193816 A>T), RS1004364381 (6:33197627 C>G,T), RS1004436689 (6:33197399 G>C,T), RS1004639676 (6:33195088 G>A), RS1005322811 (6:33201152 G>A,T), RS1005603478 (6:33201445 C>G), RS1005687293 (6:33193889 G>GGA), RS1006477418 (6:33200563 C>A,T)
Disease associations
OMIM: gene MIM:180246 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
1 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST002160_5 | Wegener’s granulomatosis | 2.000000e-50 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (3): CHEMBL1870 (SINGLE PROTEIN), CHEMBL2363070 (PROTEIN FAMILY), CHEMBL2363071 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
6 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 326,531 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1023 | BEXAROTENE | 4 | 40,951 |
| CHEMBL1071 | OXAPROZIN | 4 | 51,044 |
| CHEMBL38 | TRETINOIN | 4 | 194,008 |
| CHEMBL705 | ALITRETINOIN | 4 | 39,246 |
| CHEMBL295416 | PIRINIXIC ACID | 2 | 830 |
| CHEMBL75133 | IRX-4204 | 2 | 452 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: nhr — 2B. Retinoid X receptors
Most potent curated ligand interactions (7 total), top 7:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| LG100268 | Agonist | 8.5 | pIC50 |
| AGN194204 | Agonist | 8.44 | pIC50 |
| alitretinoin | Agonist | 8.2 | pIC50 |
| LG100754 | Antagonist | 8.0 | pIC50 |
| bexarotene | Agonist | 7.7 | pIC50 |
| [3H]9-cis-retinoic acid | Full agonist | 7.7 | pKd |
| compound 28 [Heitel et al., 2019] | Agonist | 6.51 | pEC50 |
ChEMBL bioactivities
382 potent at pChembl≥5 of 442 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
334 with measured affinity, of 1003 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-[methyl-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)amino]benzoic acid | 726704: Agonist activity at RXR (unknown origin) in presence of RAR agonist Am80 | ec50 | 0.0001 | uM |
| 4-[(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)-propylamino]benzoic acid | 726704: Agonist activity at RXR (unknown origin) in presence of RAR agonist Am80 | ec50 | 0.0001 | uM |
| tretinoin | 41913: Binding affinity for retinoic acid receptor RAR beta | ki | 0.0005 | uM |
| trans-(1R,2R)-2-[5-[3,5-bis(trifluoromethyl)phenyl]-4-phenyl-1,3-oxazol-2-yl]cyclopropane-1-carboxylic acid | 2024929: Agonist activity at full length human RXR beta expressed in HEK293T cells measured after 16 hrs by Dual-glo luciferase assay | ec50 | 0.0007 | uM |
| (2E,4E)-3-methyl-5-[(1S,2S)-2-methyl-2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]penta-2,4-dienoic acid | 167592: Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta | ec50 | 0.0008 | uM |
| (2E,4E,6Z)-7-(3-methoxy-5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-3-methylocta-2,4,6-trienoic acid | 199784: Inhibition of [3H]-Targretin binding to Retinoid X receptor RXR beta | ki | 0.0020 | uM |
| (2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-5-(3,5-difluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0024 | uM |
| (2E,4E)-3-methyl-5-[2-methyl-2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]penta-2,4-dienoic acid | 167593: Inhibition of [3H]9-cis-retinoic acid binding to baculovirus expressed retinoic acid receptor RXR-beta | kd | 0.0025 | uM |
| alitretinoin | 199801: Effective concentrations against Retinoic acid receptor RXR-beta | ec50 | 0.0026 | uM |
| (2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-3-propan-2-yl-5-thiophen-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0039 | uM |
| (2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-5-(4-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0039 | uM |
| (Z)-3-[7-[2-(2,2-difluoroethoxy)-3,5-di(propan-2-yl)phenyl]-1-benzofuran-2-yl]-2-fluorobut-2-enoic acid | 199814: Displacement of [3H]9-cis-RA from Retinoic X receptor beta | ki | 0.0040 | uM |
| (2E,4E,6Z)-7-[3,5-ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0040 | uM |
| 4-[(E)-N-hydroxy-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid | 199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay | ki | 0.0050 | uM |
| (2E,4E,6E)-7-[2-(2,2-difluoroethoxy)-3,5-bis(2-methylbutan-2-yl)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0052 | uM |
| Bexarotene | 199232: Selective activity towards retinoid X receptor-beta | ki | 0.0059 | uM |
| 4-[(E)-C-(3-bromo-5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-N-hydroxycarbonimidoyl]benzoic acid | 199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay | ki | 0.0060 | uM |
| (2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-5-(3-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0074 | uM |
| 6-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid | 199814: Displacement of [3H]9-cis-RA from Retinoic X receptor beta | ki | 0.0075 | uM |
| 4-[ethyl-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)amino]benzoic acid | 1630288: Agonist activity at human RXR binding domain and activation domain expressed in human HCT116 cells assessed as rexinoid activity incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay | ec50 | 0.0079 | uM |
| 4-[(E)-N-methoxy-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid | 199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay | ki | 0.0080 | uM |
| (2E,4E,6Z)-7-[2-butoxy-5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0082 | uM |
| (2E,4E,6Z)-7-[2-ethoxy-5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0085 | uM |
| (2E,4E,6Z)-7-(3-ethoxy-5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-3-methylocta-2,4,6-trienoic acid | 199782: Transcriptional activation of Retinoid X receptor RXR beta | ec50 | 0.0090 | uM |
| (2E,4E,6Z)-3-methyl-7-(5,5,8,8-tetramethyl-3-propoxy-6,7-dihydronaphthalen-2-yl)octa-2,4,6-trienoic acid | 199784: Inhibition of [3H]-Targretin binding to Retinoid X receptor RXR beta | ki | 0.0090 | uM |
| (2E,4E,6Z)-3-methyl-7-[3-(1,1,2,2,2-pentafluoroethyl)-5-propan-2-yl-2-propoxyphenyl]octa-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0099 | uM |
| (E)-3-[4-[3,5-ditert-butyl-2-(3-fluoropropoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acid | 199814: Displacement of [3H]9-cis-RA from Retinoic X receptor beta | ki | 0.0100 | uM |
| (E)-3-[4-[3,5-ditert-butyl-2-(2,2,2-trifluoroethoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acid | 199814: Displacement of [3H]9-cis-RA from Retinoic X receptor beta | ki | 0.0100 | uM |
| (2E,4E,6E)-7-(3,5-ditert-butylphenyl)-3-methylocta-2,4,6-trienoic acid | 199807: Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR beta | ki | 0.0102 | uM |
| (E)-3-[4-[2-ethoxy-3,5-di(propan-2-yl)phenyl]-1-benzothiophen-2-yl]but-2-enoic acid | 199814: Displacement of [3H]9-cis-RA from Retinoic X receptor beta | ki | 0.0110 | uM |
| (2E,4E,6E)-7-[3,5-ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0115 | uM |
| (E)-3-[4-[3,5-ditert-butyl-2-(3,3-difluoropropoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acid | 199814: Displacement of [3H]9-cis-RA from Retinoic X receptor beta | ki | 0.0120 | uM |
| 4-[(E)-N-ethoxy-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid | 199802: Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-beta | ec50 | 0.0120 | uM |
| (2E,4E)-6-[(6-tert-butyl-1,1-dimethyl-2,3-dihydroinden-4-yl)-propylamino]-3-methylhexa-2,4-dienoic acid | 263923: Binding affinity to RXRbeta | ki | 0.0120 | uM |
| (E)-3-[4-(3,5-ditert-butyl-2-heptoxyphenyl)-1-benzothiophen-2-yl]but-2-enoic acid | 199814: Displacement of [3H]9-cis-RA from Retinoic X receptor beta | ki | 0.0120 | uM |
| [[(2S)-1-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]phosphonic acid | 199814: Displacement of [3H]9-cis-RA from Retinoic X receptor beta | ki | 0.0120 | uM |
| (2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-3-phenyl-5-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0123 | uM |
| 6-[ethyl-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)amino]pyridine-3-carboxylic acid | 1630288: Agonist activity at human RXR binding domain and activation domain expressed in human HCT116 cells assessed as rexinoid activity incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay | ec50 | 0.0138 | uM |
| 6-[ethyl-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)amino]pyridine-3-carboxylic acid | 1630288: Agonist activity at human RXR binding domain and activation domain expressed in human HCT116 cells assessed as rexinoid activity incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay | ec50 | 0.0138 | uM |
| 4-[(E)-N-(cyanomethoxy)-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid | 199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay | ki | 0.0140 | uM |
| 4-[(E)-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)-N-prop-2-enoxycarbonimidoyl]benzoic acid | 199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay | ki | 0.0150 | uM |
| (E)-3-[4-[3,5-di(propan-2-yl)-2-propoxyphenyl]-1-benzothiophen-2-yl]but-2-enoic acid | 199814: Displacement of [3H]9-cis-RA from Retinoic X receptor beta | ki | 0.0150 | uM |
| (2E,4E)-3-methyl-5-[2-[(E)-2-(2,6,6-trimethylcyclohexen-1-yl)ethenyl]furan-3-yl]penta-2,4-dienoic acid | 199805: Inhibition of [3H]-9-cis RA binding to Retinoid X receptor RXR beta | kd | 0.0150 | uM |
| (2E,4E,6E)-7-[3,5-ditert-butyl-2-(2,2,2-trifluoroethoxy)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0155 | uM |
| (2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-5-(2-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0160 | uM |
| trans-(1S,2S)-2-[5-[3,5-bis(trifluoromethyl)phenyl]-4-phenyl-1,3-oxazol-2-yl]cyclopropane-1-carboxylic acid | 2024929: Agonist activity at full length human RXR beta expressed in HEK293T cells measured after 16 hrs by Dual-glo luciferase assay | ec50 | 0.0160 | uM |
| (E)-3-[5-[3,5-bis(trifluoromethyl)phenyl]-4-phenyl-1,3-oxazol-2-yl]-2-methylprop-2-enoic acid | 2024929: Agonist activity at full length human RXR beta expressed in HEK293T cells measured after 16 hrs by Dual-glo luciferase assay | ec50 | 0.0170 | uM |
| (2E,4E,6Z)-3-methyl-7-[5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-yl-2-propoxyphenyl]octa-2,4,6-trienoic acid | 199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | ki | 0.0172 | uM |
| 3-[4-chloro-6-(4,4-dimethyl-2,3-dihydroquinolin-1-yl)pyrimidin-2-yl]oxypropanoic acid | 2099261: Partial agonist activity at recombinant human RXR beta LBD (298 to 533 residues) expressed in Escherichia coli Rosetta incubated for 16 hrs by Gal4-hybrid reporter gene based Dual-glo luciferase assay | ec50 | 0.0180 | uM |
| 2-[ethyl-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)amino]pyrimidine-5-carboxylic acid | 1630288: Agonist activity at human RXR binding domain and activation domain expressed in human HCT116 cells assessed as rexinoid activity incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay | ec50 | 0.0182 | uM |
CTD chemical–gene interactions
78 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Alitretinoin | decreases reaction, increases activity, affects activity, affects cotreatment, increases reaction (+2 more) | 7 |
| Tretinoin | increases expression, increases activity, affects binding, affects cotreatment | 6 |
| bisphenol A | increases expression, affects binding, decreases reaction, increases activity, affects cotreatment | 5 |
| Decitabine | increases expression, decreases expression, decreases reaction | 2 |
| Valproic Acid | affects expression, decreases expression | 2 |
| 2-hydroxyphytanic acid | affects binding | 1 |
| testosterone enanthate | affects expression | 1 |
| 2,4-dichlorophenol | increases activity | 1 |
| triphenyl phosphate | affects expression | 1 |
| diethyl phthalate | affects binding | 1 |
| triphenyltin hydroxide | affects activity, affects binding | 1 |
| diisononyl phthalate | affects binding | 1 |
| mono-(2-ethylhexyl)phthalate | affects binding | 1 |
| butyraldehyde | decreases expression | 1 |
| dinonylphthalate | affects binding | 1 |
| 2,4,6-trichlorophenol | affects binding, decreases reaction, increases activity | 1 |
| dimethyl phthalate | affects binding | 1 |
| manganese chloride | decreases expression, increases abundance | 1 |
| di-n-hexyl phthalate | affects binding | 1 |
| butylbenzyl phthalate | affects binding | 1 |
| 4-hydroxy-2-nonenal | decreases expression | 1 |
| didecyl phthalate | affects binding | 1 |
| nickel sulfate | increases expression | 1 |
| phthalic acid | affects binding | 1 |
| di-n-pentyl phthalate | affects binding | 1 |
| 2-tert-butylphenol | increases activity | 1 |
| tetrachlorodian | affects binding, decreases reaction, increases activity | 1 |
| diisodecyl phthalate | affects binding | 1 |
| 3,4-dichlorophenol | increases activity | 1 |
| pentanal | decreases expression | 1 |
ChEMBL screening assays
211 unique, capped per target: 183 binding, 28 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1021934 | Binding | Activity at Gal4-tagged human RXRbeta receptor expressed in human HeLa cells assessed as relative transcriptional activity by luciferase reporter assay relative to CD3254 | Modulating retinoid X receptor with a series of (E)-3-[4-hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic acids and their 4-alkoxy isomers. — J Med Chem |
| CHEMBL1021935 | Functional | Antagonist activity at Gal4-tagged human RXRbeta receptor expressed in human HeLa cells assessed as inhibition of CD3254-induced transcription at >=10 uM by luciferase reporter assay | Modulating retinoid X receptor with a series of (E)-3-[4-hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic acids and their 4-alkoxy isomers. — J Med Chem |
Cellosaurus cell lines
9 cell lines: 5 cancer cell line, 3 embryonic stem cell, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_A5Z7 | SEES3-1V human RXRB, clone1 | Embryonic stem cell | Male |
| CVCL_A5Z8 | SEES3-1V human RXRB, clone2 | Embryonic stem cell | Male |
| CVCL_A5Z9 | SEES3-1V human RXRB, clone3 | Embryonic stem cell | Male |
| CVCL_D1QF | Abcam K-562 RXRB KO | Cancer cell line | Female |
| CVCL_D2M1 | Abcam Raji RXRB KO | Cancer cell line | Male |
| CVCL_LF54 | GeneBLAzer RXRbeta-UAS-bla HEK 293T | Transformed cell line | Female |
| CVCL_TJ89 | HAP1 RXRB (-) 1 | Cancer cell line | Male |
| CVCL_TJ90 | HAP1 RXRB (-) 2 | Cancer cell line | Male |
| CVCL_WQ49 | Abcam Jurkat RXRB KO | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Targeted by drugs: Alitretinoin, Bexarotene
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): granulomatosis with polyangiitis