Retinoic acid receptor-γ
Target has curated data in GtoImmuPdb
Target id: 592
Nomenclature: Retinoic acid receptor-γ
Systematic Nomenclature: NR1B3
Family: 1B. Retinoic acid receptors
Contents:
- Gene and Protein Information
- Previous and Unofficial Names
- Database Links
- Selected 3D Structures
- Natural/Endogenous Ligands
- Agonists
- Antagonists
- Immunopharmacology Comments
- Immuno Process Associations
- DNA Binding
- Co-binding Partners
- Main Co-regulators
- Main Target Genes
- Tissue Distribution
- Functional Assays
- Physiological Consequences of Altering Gene Expression
- Phenotypes, Alleles and Disease Models
- Gene Expression and Pathophysiology
- Biologically Significant Variants
- References
- How to cite this page
Gene and Protein Information  |
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| Species | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 454 | 12q13.13 | RARG | retinoic acid receptor gamma | 29,36,46 |
| Mouse | 458 | 15 57.4 cM | Rarg | retinoic acid receptor, gamma | 30,46 |
| Rat | 458 | 7q36 | Rarg | retinoic acid receptor, gamma | 38,43,46 |
| Previous and Unofficial Names |
| RARC | RARγ | RAR gamma 2 | retinoic acid receptor |
| Database Links |
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| Alphafold | P13631 (Hs), P18911 (Mm) |
| CATH/Gene3D | 3.30.50.10 |
| ChEMBL Target | CHEMBL2003 (Hs), CHEMBL4177 (Mm) |
| DrugBank Target | P13631 (Hs) |
| Ensembl Gene | ENSG00000172819 (Hs), ENSMUSG00000001288 (Mm), ENSRNOG00000012499 (Rn) |
| Entrez Gene | 5916 (Hs), 19411 (Mm), 685072 (Rn) |
| Human Protein Atlas | ENSG00000172819 (Hs) |
| KEGG Gene | hsa:5916 (Hs), mmu:19411 (Mm), rno:685072 (Rn) |
| OMIM | 180190 (Hs) |
| Pharos | P13631 (Hs) |
| RefSeq Nucleotide | NM_001042728 (Hs), NM_001042727 (Mm), NM_011244 (Mm), NM_001135249 (Rn), NM_001135250 (Rn) |
| RefSeq Protein | NP_001036193 (Hs), NP_000957 (Hs), NP_035374 (Mm), NP_001036192 (Mm), NP_001128721 (Rn), NP_001128722 (Rn) |
| SynPHARM |
6292 (in complex with BMS270394) 79008 (in complex with tretinoin) 6288 (in complex with tretinoin) 85230 (in complex with trifarotene) |
| UniProtKB | P13631 (Hs), P18911 (Mm) |
| Wikipedia | RARG (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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Agonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Although all-trans-retinoic acid has high affinity for all retinoic acid receptor isoforms, it has approximately 6-8 times higher affinity for the γ isoform [8]. Adapalene is selective for the β and γ RARs over the α isoform [7]. |
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| 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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| AGN193109 was the first described inverse agonist. CD2665 is a RARβ/γ antagonist. No pure RARγ-selective antagonist has been reported so far. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Immunopharmacology Comments |
| Retinoid drugs reduce the proinflammatory factors and disrupt the immunoinflammatory cascade associated with acne vulgaris. RARγ is one of the molecular targets of anti-acne retinoid family drugs. RARγ-selective retinoid derivatives are being investigated as topical agents, which are expected to offer a more favourable clinical profile compared to the dual RARβ/γ drugs currently used in the clinic. |
| Immuno Process Associations | ||
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| DNA Binding |
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| DNA Binding Comments | |||||||
| The classical sequence is a 5-pb-spaced direct repeat (DR5). In DR5 and DR2 RXR occupies the 5’ element. | |||||||
| Co-binding Partners |
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| Name | Interaction | Effect | Reference |
| AP1 | Functional | RARg inhibits AP-1 driven transactivation | 11,37,49,56-57 |
| cdk7/TFIIH | Physical, Functional | TFIIH phosphorylates RARg2 in its A/B region (ser 68) by cdk7 subunit. | 2,52 |
| p38MAPK | Functional | p38MAPK is required for RA-induced RARg degradation and transactivation | 24-25,52 |
| SUG1 | Physical, Functional | SUG1 is required for RA-induced RARg degradation and transactivation | 24-25,52 |
| vinexin beta | Physical, Functional | Interacts with AF-1 domain of RARg and repress RARgamma-mediated transcription. | 5 |
| Main Co-regulators |
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| Name | Activity | Specific | Ligand dependent | AF-2 dependent | Comments | References |
| NCOR1 | Co-repressor | No | No | No | Binding of an agonist to RARg causes NCoR dissociation | 18,28,47,68 |
| NCOA1 | Co-activator | No | Yes | Yes | A member of the p160 family | 38,47,50 |
| NCOA2 | Co-activator | No | Yes | Yes | A member of the p160 family | 47,65-66 |
| NCOA3 | Co-activator | No | Yes | Yes | A member of the p160 family | 9,18,41 |
| NCOR2 | Co-repressor | No | No | No | Binding of an agonist to RARg causes SMRT dissociation | 10,55-56 |
| Main Target Genes |
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| Name | Species | Effect | Technique | Comments | References |
| RARβ2 | Human | Activated | EMSA | This gene has been shown to be activated in all species (human,mouse,rat). The promoter harbors a DR5 element | 12-13,19 |
| Hoxa1 | Mouse | Activated | The promoter harbors a DR5 element | 12,16,38 | |
| Rbp1 | Mouse | Activated | The promoter harbors a DR2 element. | 12,58 | |
| Crabp2 | Mouse | Activated | EMSA | The promoter harbors a DR2 element. | 12,17 |
| Lamb1-1 | Mouse | Activated | EMSA | The promoter harbors a DR5 element. | 63 |
| Tissue Distribution
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| Tissue Distribution Comments | ||||||||||
| The different RARγ isoforms exhibit specific expression patterns. | ||||||||||
| 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 specific RARγ2 null mutants are apparently normal, and specific RARγ a null mutant exhibited growth deficiency, malformations of cervical vertebrae and abnormal differentiation of granular keratinocytes. | ||||||||||
| Phenotypes, Alleles and Disease Models
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Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Gene Expression and Pathophysiology
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| Biologically Significant Variants
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References
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1B. Retinoic acid receptors: Retinoic acid receptor-γ. Last modified on 26/06/2018. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=592.
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