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Target not currently curated in GtoImmuPdb
Target id: 591
Nomenclature: Retinoic acid receptor-β
Systematic Nomenclature: NR1B2
Family: 1B. Retinoic acid receptors
Gene and Protein Information | |||||
Species | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 455 | 3p24.2 | RARB | retinoic acid receptor beta | 3,32 |
Mouse | 482 | 14 7.08 cM | Rarb | retinoic acid receptor, beta | 32,34,53-54 |
Rat | 291 | 15p16 | Rarb | retinoic acid receptor, beta | 32 |
Gene and Protein Information Comments | |||||
The 448 aa human isoform (1, a.k.a. β2) is the predominant transcript. Other alternatively spliced transcripts are described, including the 455 aa isoform 3 (a.k.a. β1; NP_001277145). |
Previous and Unofficial Names |
HAP | HBV-activated protein | RAR beta 2 | retinoic acid receptor |
Database Links | |
Alphafold | P10826 (Hs), P22605 (Mm), D3ZFD9 (Rn) |
CATH/Gene3D | 3.30.50.10 |
ChEMBL Target | CHEMBL2008 (Hs), CHEMBL3266 (Mm) |
DrugBank Target | P10826 (Hs) |
Ensembl Gene | ENSG00000077092 (Hs), ENSMUSG00000017491 (Mm), ENSRNOG00000024061 (Rn) |
Entrez Gene | 5915 (Hs), 218772 (Mm), 24706 (Rn) |
Human Protein Atlas | ENSG00000077092 (Hs) |
KEGG Gene | hsa:5915 (Hs), mmu:218772 (Mm), rno:24706 (Rn) |
OMIM | 180220 (Hs) |
Orphanet | ORPHA368114 (Hs) |
Pharos | P10826 (Hs) |
RefSeq Nucleotide | NM_016152 (Hs), NM_011243 (Mm), NM_031529 (Rn) |
RefSeq Protein | NP_000956 (Hs), NP_057236 (Hs), NP_035373 (Mm), NP_113717 (Rn) |
SynPHARM |
79006 (in complex with tretinoin) 6287 (in complex with tretinoin) 6285 (in complex with TTNPB) |
UniProtKB | P10826 (Hs), P22605 (Mm), D3ZFD9 (Rn) |
Wikipedia | RARB (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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific agonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Agonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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. BMS641 is a partial RARβ-selective agonist. However no fully RARβ-selective agonist has been reported so far. Although tazarotene has high affinity for all retinoic acid receptor isoforms, it has roughly 5-8 times higher affinity for the β isoform [6]. Adapalene is selective for the β and γ RARs over the α isoform [5]. |
Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Antagonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
To date, no pure RARβ-selective antagonist has been reported. Both AGN193109 and BMS493 inverse agonists can induce corepressor association with RARβ instead of RARα. |
Co-binding Partners | |||
Name | Interaction | Effect | Reference |
AP1 | Functional | RARb inhibits AP-1 driven transactivation | 36 |
Main Co-regulators | ||||||
Name | Activity | Specific | Ligand dependent | AF-2 dependent | Comments | References |
NCOA1 | Co-activator | No | Yes | Yes | A member of the p160 family | 11,37 |
MED1 | Co-activator | No | Yes | Yes | A member of the DRIP/TRAP/SMCC complex | 25,33,39,52 |
NCOA3 | Co-activator | No | Yes | Yes | A member of the p160 family | 7,11,26 |
NCOA2 | Co-activator | No | Yes | Yes | A member of the p160 family | 12,24,46 |
Tissue Distribution | ||||||||||
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Tissue Distribution Comments | ||||||||||
Similar distribution patterns are seen in the mouse and rat. |
Physiological Consequences of Altering Gene Expression | ||||||||||
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Physiological Consequences of Altering Gene Expression Comments | ||||||||||
Note that the specific RARβ1/β3 null mutants are apparently normal, and the specific RARβ2/β4 null mutants exhibited persistence and hyperplasia of the primary vitreous body. |
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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General Comments |
Using F9 RARβ2 null cells, some genes have been identified that require RARβ2 for their regulation by ATRA in F9 cells [27,55]. In contrast to RARα, unliganded RARβ poorly interacts with both NCoR and SMRT corepressors. |
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1B. Retinoic acid receptors: Retinoic acid receptor-β. Last modified on 10/07/2023. Accessed on 09/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=591.