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Target id: 593
Nomenclature: Peroxisome proliferator-activated receptor-α
Systematic Nomenclature: NR1C1
Gene and Protein Information | |||||
Species | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 468 | 22q13.31 | PPARA | peroxisome proliferator activated receptor alpha | 63 |
Mouse | 468 | 15 40.42 cM | Ppara | peroxisome proliferator activated receptor alpha | 33 |
Rat | 468 | 7q34 | Ppara | peroxisome proliferator activated receptor alpha | 27 |
Previous and Unofficial Names |
NUC1 | nuclear receptor subfamily 1 group C member 1 | PPARalpha | PPAR |
Database Links | |
Alphafold | Q07869 (Hs), P23204 (Mm), P37230 (Rn) |
CATH/Gene3D | 3.30.50.10 |
ChEMBL Target | CHEMBL239 (Hs), CHEMBL2128 (Mm), CHEMBL2129 (Rn) |
DrugBank Target | Q07869 (Hs) |
Ensembl Gene | ENSG00000186951 (Hs), ENSMUSG00000022383 (Mm), ENSRNOG00000021463 (Rn) |
Entrez Gene | 5465 (Hs), 19013 (Mm), 25747 (Rn) |
Human Protein Atlas | ENSG00000186951 (Hs) |
KEGG Gene | hsa:5465 (Hs), mmu:19013 (Mm), rno:25747 (Rn) |
OMIM | 170998 (Hs) |
Pharos | Q07869 (Hs) |
RefSeq Nucleotide | NM_001001928 (Hs), NM_001113418 (Mm), NM_011144 (Mm), NM_013196 (Rn) |
RefSeq Protein | NP_001001928 (Hs), NP_035274 (Mm), NP_037328 (Rn) |
SynPHARM |
6299 (in complex with GW409544) 7986 (in complex with GW6471) 6309 (in complex with pirinixic acid) |
UniProtKB | Q07869 (Hs), P23204 (Mm), P37230 (Rn) |
Wikipedia | PPARA (Hs) |
Selected 3D Structures | |||||||||||||
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Natural/Endogenous Ligands |
LTB4 |
pristanic acid |
8S-HETE |
Comments: LTB4, fatty acids and eisosanoids are natural ligands |
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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Pterostilbene, tetradecylglycidic acid and ortylthiopropionic acid (OTP) are also known agonists [10,58]. Fenofibrate is selective for PPARα. In a cell-based reporter transactivation assay fenofibrate is active at PPARα with an EC50 of 30μM, compared to 300μM vs. PPARγ [29]. This assay does not address the contribution to functional activity made by the active metabolite of fenofibrate, fenofibric acid. |
Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific antagonist tables |
Immuno Process Associations | ||
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Co-binding Partners | |||
Name | Interaction | Effect | Reference |
RXR | Physical, Functional | DNA binding | 42 |
Main Co-regulators | ||||||
Name | Activity | Specific | Ligand dependent | AF-2 dependent | Comments | References |
NCOR1 | Co-repressor | No | No | No | 10,13,16 | |
MED1 | Co-activator | No | Yes | Yes | 83 | |
NCOA1 | Co-activator | No | Yes | No | 82 | |
NCOA6 | Co-activator | No | Yes | Yes | 7,81 | |
HADHA | Co-activator | No | No | No | 36 | |
SMARCA2 | Co-activator | No | No | Yes | 65 | |
NRIP1 | Co-repressor | No | Yes | Yes | 35,52,75 | |
CITED2 | Co-activator | No | Yes | Yes | 66 | |
NCOA3 | Co-activator | No | No | Yes | 53 | |
PPARGC1A | Co-activator | No | No | No | 68 | |
PPARGC1B | Co-activator | No | No | No | 68 | |
CREBBP | Co-activator | No | Yes | Yes | There are contradicting results for ligand-dependency | 15,80 |
Main Target Genes | |||||
Name | Species | Effect | Technique | Comments | References |
CPTI: carnitine palmitoyl transferase I | Human | Activated | Transient transfection | 2,50,76 | |
MCAD (medium chain acyl-coA dehydrogenase) | Rat | Activated | Transient transfection | 25 | |
Acyl-CoA oxidase | Rat | Activated | Transient transfection | 49,67 | |
Fiat ( fasting induced adipose tissue factor) | Mouse | Activated | 41 | ||
Bifunctional enzyme | Mouse | Activated | Transient transfection | 49 | |
Slc27a1 | Mouse | Activated | Transient transfection, EMSA | FATP, fatty acid transport protein | 21 |
Apolipoprotein A-II | Mouse | Activated | Transient transfection, EMSA | negative regulation of A-I | 69 |
G0/G1 switch gene 2 (G0S2) | Mouse | Activated | 78 | ||
Liver fatty acid binding protein | Mouse | Activated | 10,34 |
Tissue Distribution | ||||||||||
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Phenotypes, Alleles and Disease Models | Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Clinically-Relevant Mutations and Pathophysiology | ||||||||||
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Gene Expression and Pathophysiology | ||||||||||||
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