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Target id: 610
Nomenclature: Retinoid X receptor-α
Systematic Nomenclature: NR2B1
Family: 2B. Retinoid X receptors
Gene and Protein Information | |||||
Species | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 462 | 9q34.2 | RXRA | retinoid X receptor alpha | 2,32,48 |
Mouse | 467 | 2 19.38 cM | Rxra | retinoid X receptor alpha | 31,43-44,47 |
Rat | 467 | 3p12 | Rxra | retinoid X receptor alpha | 25 |
Previous and Unofficial Names |
RXRα | nuclear receptor subfamily 2 group B member 1 | retinoic acid receptor RXR-alpha | retinoid X receptor, alpha |
Database Links | |
Alphafold | P19793 (Hs), P28700 (Mm), Q05343 (Rn) |
CATH/Gene3D | 3.30.50.10 |
ChEMBL Target | CHEMBL2061 (Hs), CHEMBL3084 (Mm), CHEMBL4431 (Rn) |
DrugBank Target | P19793 (Hs) |
Ensembl Gene | ENSG00000186350 (Hs), ENSMUSG00000015846 (Mm), ENSRNOG00000009446 (Rn) |
Entrez Gene | 6256 (Hs), 20181 (Mm), 25271 (Rn) |
Human Protein Atlas | ENSG00000186350 (Hs) |
KEGG Gene | hsa:6256 (Hs), mmu:20181 (Mm), rno:25271 (Rn) |
OMIM | 180245 (Hs) |
Pharos | P19793 (Hs) |
RefSeq Nucleotide | NM_002957 (Hs), NM_011305 (Mm), NM_012805 (Rn) |
RefSeq Protein | NP_002948 (Hs), NP_035435 (Mm), NP_036937 (Rn) |
SynPHARM |
6485 (in complex with alitretinoin) 6486 (in complex with bexarotene) |
UniProtKB | P19793 (Hs), P28700 (Mm), Q05343 (Rn) |
Wikipedia | RXRA (Hs) |
Selected 3D Structures | |||||||||||||
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Natural/Endogenous Ligands |
alitretinoin |
docosahexaenoic acid |
Download all structure-activity data for this target as a CSV file
Agonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Agonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
It is unclear whether docosahexaenoic acid and phytanic acid are bona fide endogenous ligands for RXR. |
Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Antagonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
NB: LG100754 is a RXR:RXR antagonist, a RXR:PPARalpha agonist but also functions as a RXR:PPARgamma agonist [11]. |
Immuno Process Associations | ||
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Co-binding Partners | |||
Name | Interaction | Effect | Reference |
Pregnane X receptor | Physical, Functional | DNA binding | 5-6,37,42 |
Thyroid hormone receptor-α | Physical, Functional | DNA binding (this is also true for TRβ) | 9,27,44 |
Vitamin D receptor | Physical, Functional | DNA binding | 9,27 |
Retinoic acid receptor-α | Physical, Functional | DNA binding (also all the other RARs) | 4,9,26-27,38,44,75 |
Peroxisome proliferator-activated receptor-α | Physical, Functional | DNA binding | 38,67 |
Liver X receptor-α | Physical, Functional | DNA binding (and also all other LXRs) | 23,65,72-73 |
Farnesoid X receptor | Physical, Functional | DNA binding | 61 |
Constitutive androstane receptor | Physical, Functional | DNA binding | 3,17 |
Nuclear receptor related 1 | Physical, Functional | DNA binding | 57 |
Nerve Growth factor IB | Physical, Functional | DNA binding | 24,57 |
Main Co-regulators | ||||||
Name | Activity | Specific | Ligand dependent | AF-2 dependent | Comments | References |
NCOA1 | Co-activator | No | Yes | Yes | 52,56 | |
NCOA2 | Co-activator | No | Yes | Yes | 68-69 | |
NCOA3 | Co-activator | No | Yes | - | 15,52 | |
PPARGC1A | Co-activator | No | Yes | Yes | 19 | |
MED1 | Co-activator | No | Yes | Yes | 52,74 | |
TBP | Co-activator | No | Yes | Yes | 39,52,60 | |
TAF4 | Co-activator | No | Yes | Yes | 39,52,60 | |
TAF11 | Co-activator | No | Yes | Yes | 51 | |
CREBBP | Co-activator | No | Yes | Yes | 12,33 | |
EP300 | Co-activator | No | Yes | Yes | 12 |
Tissue Distribution | ||||||||||
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Tissue Distribution Comments | ||||||||||
RXRa2, an isoform, is specifically expressed in testis. Similar expression patterns are also seen in rodents. |
Functional Assays | ||||||||||
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Physiological Consequences of Altering Gene Expression | ||||||||||
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Phenotypes, Alleles and Disease Models | Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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General Comments |
Through its heterodimeric interaction with many other nuclear receptors, RXRα may play a role in a wide variety of diseases as well as in the control of multiple target genes. |
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2B. Retinoid X receptors: Retinoid X receptor-α. Last modified on 28/03/2019. Accessed on 01/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=610.