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Target not currently curated in GtoImmuPdb
Target id: 590
Nomenclature: Retinoic acid receptor-α
Systematic Nomenclature: NR1B1
Family: 1B. Retinoic acid receptors
Gene and Protein Information ![]() |
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Species | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 462 | 17q21.2 | RARA | retinoic acid receptor alpha | 49,55 |
Mouse | 462 | 11 62.76 cM | Rara | retinoic acid receptor, alpha | 40-41,49,72 |
Rat | 459 | 10 | Rara | retinoic acid receptor, alpha | 1,49 |
Previous and Unofficial Names ![]() |
RAR alpha 1 | RAR | RARα | retinoic acid receptor |
Database Links ![]() |
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CATH/Gene3D | 3.30.50.10 |
ChEMBL Target | CHEMBL2055 (Hs), CHEMBL2792 (Mm) |
DrugBank Target | P10276 (Hs) |
Ensembl Gene | ENSG00000131759 (Hs), ENSMUSG00000037992 (Mm), ENSRNOG00000009972 (Rn) |
Entrez Gene | 5914 (Hs), 19401 (Mm), 24705 (Rn) |
Human Protein Atlas | ENSG00000131759 (Hs) |
KEGG Gene | hsa:5914 (Hs), mmu:19401 (Mm), rno:24705 (Rn) |
OMIM | 180240 (Hs) |
Orphanet | ORPHA118227 (Hs) |
Pharos | P10276 (Hs) |
RefSeq Nucleotide | NM_001145302 (Hs), NM_009024 (Mm), NM_001177302 (Mm), NM_001177303 (Mm), NM_001176528 (Mm), NM_031528 (Rn) |
RefSeq Protein | NP_001138773 (Hs), NP_001019980 (Hs), NP_033050 (Mm), NP_113716 (Rn) |
SynPHARM |
6273 (in complex with BMS614) 83084 (in complex with Ro 40-6055) 7547 (in complex with Ro 40-6055) 79003 (in complex with tretinoin) |
UniProtKB | P10276 (Hs), P11416 (Mm) |
Wikipedia | RARA (Hs) |
Selected 3D Structures ![]() |
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Natural/Endogenous Ligands ![]() |
tretinoin |
Download all structure-activity data for this target as a CSV file
Agonists ![]() |
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Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific agonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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All-trans-retinoic acid is the most potent endogenous retinoid. The existence of 9-cis retinoic acid as a natural bioactive retinoid remains to be established. Synthetic compounds (reported above) are not metabolized by CYP26. No significant species variation has been reported. The possibility of establishing a hydrogen bond between an amino group present in the linker of the identified RARα-selective agonists and the RARα-specific Ser232 is predicted to favour RARα selectivity. Adapalene is selective for the β and γ RARs over the α isoform [10]. |
Antagonists ![]() |
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Key to terms and symbols | View all chemical structures | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Antagonist Comments | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
No significant species variation has been reported. |
Immuno Process Associations | |||||||||||||||
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Co-binding Partners ![]() |
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Name | Interaction | Effect | Reference |
cyclin H/cdk7/TFIIH | Physical, Functional | TFIIH phosphorylates RARa1 in its A/B region (ser 77) by cdk7 subunit. | 7,56-57 |
AP-1 | Physical, Functional | RAR inhibits AP-1 driven transactivation and AP-1 represses RAR-mediated transcription | 13,36,52,62,73 |
CRABPII | Physical, Functional | Indispensable to RARα-mediated transcription from the RARα2 | 21 |
PARP-1 | Physical, Functional | Indispensable to RARα-mediated transcription from the RARα2 | 54 |
Main Co-regulators ![]() |
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Name | Activity | Specific | Ligand dependent | AF-2 dependent | Comments | References |
NCOA1 | Co-activator | No | Yes | Yes | A member of the p160 family | 53,70 |
NCOR1 | Co-repressor | No | No | No | Binding of an agonist to RARa causes NCoR dissociation | 30,50 |
EP300 | Co-activator | No | Yes | Yes | A common cointegrator | 28 |
CREBBP | Co-activator | No | Yes | Yes | A common cointegrator | 28 |
MED1 | Co-activator | No | Yes | Yes | A member of the DRIP/TRAP/SMCC complex | 28,37,47 |
NCOA3 | Co-activator | No | Yes | Yes | A member of the p160 family | 12 |
NCOA2 | Co-activator | No | Yes | Yes | A member of the p160 family | 69 |
NCOR2 | Co-repressor | No | No | No | Binding of an agonist to RARa causes SMRT dissociation | 13,61,71 |
Main Target Genes ![]() |
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Name | Species | Effect | Technique | Comments | References |
CYP26 | Human | Activated | Footprint, Transient transfection,ChIP,EMSA | CYP26 is also activated by RARa in mouse and rat. Note: promoter harbors a DR5 element. | 45 |
RARB | Human | Activated | Footprint, Transient transfection,ChIP,EMSA | Activation is seen across all species including mouse and rat. Note: promoter harbors a DR5 element. | 14,16,18,26 |
Crabp2 | Mouse | Activated | Transient transfection, EMSA | Promoter harbors a DR2 element. | 16,25 |
Hoxa1 | Mouse | Activated | Promoter harbors a DR5 element. | 16,24,38 | |
Rbp1 | Mouse | Activated | Transient transfection | Promoter harbors a DR2 element. | 16,63 |
Tissue Distribution ![]() |
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Tissue Distribution Comments | ||||||||
Ubiquitous distribution pattern of the Rarα1 is also reported in both the mouse and rat. |
Functional Assays ![]() |
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Physiological Consequences of Altering Gene Expression ![]() |
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Physiological Consequences of Altering Gene Expression Comments | ||||||||||
Note that both the specific RARα1 null and RARα2 null mutants are apparently normal. |
Phenotypes, Alleles and Disease Models ![]() |
Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Clinically-Relevant Mutations and Pathophysiology ![]() |
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Biologically Significant Variants ![]() |
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1B. Retinoic acid receptors: Retinoic acid receptor-α. Last modified on 10/01/2020. Accessed on 19/01/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=590.