Therapeutic Target Details
| Target ID: | T03 |
| Target Name: | Peroxisome proliferator-activated receptor alpha |
| Synonyms: | PPARA; PPAR-α; PPAR-alpha; NR1C1; Nuclear receptor subfamily 1 group C member 1 |
| GENE: | PPARA |
| Action: | agonist |
| Class: | Nuclear hormone receptor |
| UniProtKB ID: | Q07869 |
| Entry Name: | PPARA_HUMAN |
| Related Drugs: | Bezafibrate; DHA; Elafibranor; Epanova; Fenofibrate; Omega 3 PUFA; Rosiglitazone; Gemfibrozil |
| Mechanism: | Peroxisome proliferator activated receptor-α (PPARα) activity is associated with increased energy burning and reduced fat storage in the liver. PPARα upregulates a number of genes that play roles in fatty acid oxidation and in phospholipid remodeling, and it inhibits hepatic inflammatory processes. |
| Reference (PMIDs): | 24524207 |
| Drug ID | Drug Name | Type | DrugBank ID | Targets | Category | Latest Progress | |
|---|---|---|---|---|---|---|---|
| D033 | Bezafibrate | Chemical drug | DB01393 | PPARA agonist; PPARD agonist; PPARG agonist; NR1I2 partial agonist | Improve insulin resistance; Anti-inflammatory | Under clinical trials | Details |
| D105 | DHA | Chemical drug | DB03756 | PPARA ligand; PPARG ligand | Anti-inflammatory | Under clinical trials | Details |
| D119 | Elafibranor | Chemical drug | DB05187 | PPARA; PPARD; PPARG | Anti-inflammatory | Failed in clinical trials | Details |
| D125 | Epanova | Chemical drug | DB11133 | PPARG ligand; PPARA activator | Enhance lipid metabolism | Under clinical trials | Details |
| D133 | Fenofibrate | Chemical drug | DB01039 | PPARA agonist; NR1I2 partial agonist | Anti-inflammatory | Under clinical trials | Details |
| D258 | Omega 3 PUFA | Chemical drug | DB11133 | PPARG ligand; PPARA activator | Hypolipidemic drug | Under clinical trials | Details |
| D311 | Rosiglitazone | Chemical drug | DB00412 | PPARG agonist; PPARA; PPARD | Improve insulin resistance | Failed in clinical trials | Details |
| D406 | Gemfibrozil | Chemical drug | DB01241 | PPARA agonist; SLCO1B1 inhibitor; SLC22A8 inhibitor; SLCO2B1 inhibitor; SLCO1B3 inhibitor | Hypolipidemic drug | Under investigation | Details |
| D527 | EPA/DHA | Supplement | DB11133 | -- | -- | Under clinical trials | Details |
| Candidate ID | Source ID | Source Type | Compound Type | Candidate Name | Inclusion Criteria | |
|---|---|---|---|---|---|---|
| R0043 | DB00132 | approved; investigational; nutraceutical | small molecule | alpha-Linolenic acid | Therapeutic strategy associated | Details |
| R0056 | DB00159 | approved; nutraceutical | small molecule | Icosapent | Therapeutic strategy associated | Details |
| R0112 | DB00313 | approved; investigational | small molecule | Valproic acid | Therapeutic strategy associated | Details |
| R0117 | DB00328 | approved; investigational | small molecule | Indomethacin | Therapeutic strategy associated | Details |
| R0197 | DB00573 | approved | small molecule | Fenoprofen | Target associated | Details |
| R0226 | DB00636 | approved; investigational | small molecule | Clofibrate | Target associated | Details |
| R0385 | DB01050 | approved | small molecule | Ibuprofen | Target associated | Details |
| R0413 | DB01118 | approved; investigational | small molecule | Amiodarone | Target associated | Details |
| R0552 | DB01708 | approved; investigational; nutraceutical | small molecule | Prasterone | Target associated | Details |
| R0556 | DB01890 | experimental | small molecule | N,N-Bis(3-(D-gluconamido)propyl)deoxycholamide | Target associated | Details |
| Compound ID | Source ID | Source Type | Compound Name | Molecular Weight | Molecular Formula | Molecular Species | |
|---|---|---|---|---|---|---|---|
| B000028 | CHEMBL101123 | Small molecule | -- | 661.6 | C33H29F6N3O5 | ACID | Details |
| B000055 | CHEMBL1017 | Small molecule | TELMISARTAN | 514.63 | C33H30N4O2 | ACID | Details |
| B000066 | CHEMBL102004 | Small molecule | -- | 649.55 | C31H28F9NO4 | ACID | Details |
| B000106 | CHEMBL104246 | Small molecule | -- | 436.51 | C25H28N2O5 | ACID | Details |
| B000116 | CHEMBL104494 | Small molecule | -- | 444.49 | C25H24N4O4 | ACID | Details |
| B000131 | CHEMBL104850 | Small molecule | -- | 416.48 | C25H24N2O4 | ACID | Details |
| B000169 | CHEMBL106256 | Small molecule | -- | 376.84 | C20H21ClO5 | ACID | Details |
| B000180 | CHEMBL106666 | Small molecule | GW7845 | 500.55 | C29H28N2O6 | ACID | Details |
| B000193 | CHEMBL1071 | Small molecule | OXAPROZIN | 293.32 | C18H15NO3 | ACID | Details |
| B000199 | CHEMBL107367 | Small molecule | FARGLITAZAR | 546.62 | C34H30N2O5 | ACID | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00006 | 35256934 | Acta Pharm Sin B | Metabolic dysregulation and emerging therapeutical targets for hepatocellular carcinoma. | Details |
| A00547 | 35051553 | Mol Cell Endocrinol | Pdcd4 promotes lipid deposition by attenuating PPARα-mediated fatty acid oxidation in hepatocytes. | Details |
| A00595 | 35035496 | Evid Based Complement Alternat Med | Lanzhang Granules Ameliorate Nonalcoholic Fatty Liver Disease by Regulating the PPARα Signaling Pathway. | Details |
| A00623 | 35024308 | Acta Pharm Sin B | Proteomics and metabolic phenotyping define principal roles for the aryl hydrocarbon receptor in mouse liver. | Details |
| A00725 | 34988225 | Biomed Res Int | Target Deconvolution of Fenofibrate in Nonalcoholic Fatty Liver Disease Using Bioinformatics Analysis. | Details |
| A01024 | 34900534 | Acta Pharm Sin B | Integrative lipidomic and transcriptomic study unravels the therapeutic effects of saikosaponins A and D on non-alcoholic fatty liver disease. | Details |
| A01186 | 34836021 | Nutrients | Euphausia pacifica (North Pacific Krill): Review of Chemical Features and Potential Benefits of 8-HEPE against Metabolic Syndrome, Dyslipidemia, NAFLD, and Atherosclerosis. | Details |
| A01775 | 34621326 | Evid Based Complement Alternat Med | A Novel Identified Peptide Hormone "Metabolitin" Attenuates Lipid Absorption in the Small Intestine of Diabetic Mice with Nonalcoholic Fatty Liver Disease by Regulating Neurotensin and AMPK Signaling Pathway. | Details |
| A02310 | 34425199 | Int J Biochem Cell Biol | Sulfated glucuronomannan hexasaccharide G6S1 enhanced lipolysis and lipophagy via PPARα pathway. | Details |
| A02443 | 34370218 | Clin J Gastroenterol | Efficacy of elafibranor in patients with liver abnormalities especially non-alcoholic steatohepatitis: a systematic review and meta-analysis. | Details |
| A02757 | 34257694 | Evid Based Complement Alternat Med | Alleviative Effect of Ruellia tuberosa L. on Insulin Resistance and Abnormal Lipid Accumulation in TNF-α-Treated FL83B Mouse Hepatocytes. | Details |
| A02937 | 34191493 | Anal Chem | Exploring the Changes of Peroxisomal Polarity in the Liver of Mice with Nonalcoholic Fatty Liver Disease. | Details |
| A03020 | 34161164 | J Med Food | Protective Role of Dietary Capsanthin in a Mouse Model of Nonalcoholic Fatty Liver Disease. | Details |
| A03551 | 33960342 | Food Funct | Functional milk fat enriched in conjugated linoleic acid prevented liver lipid accumulation induced by a high-fat diet in male rats. | Details |
| A03605 | 33934381 | Hepatology | Hepatic Small Ubiquitin-Related Modifier (SUMO)-Specific Protease 2 Controls Systemic Metabolism Through SUMOylation-Dependent Regulation of Liver-Adipose Tissue Crosstalk. | Details |
| A04045 | 33777674 | Acta Pharm Sin B | S-Allylmercaptocysteine improves alcoholic liver disease partly through a direct modulation of insulin receptor signaling. | Details |
| A04128 | 33746742 | Front Pharmacol | Liraglutide Alleviates Hepatic Steatosis and Liver Injury in T2MD Rats via a GLP-1R Dependent AMPK Pathway. | Details |
| A04989 | 33422644 | Mol Metab | Neonatal overfeeding during lactation rapidly and permanently misaligns the hepatic circadian rhythm and programmes adult NAFLD. | Details |
| A05052 | 33392801 | Curr Atheroscler Rep | Selective Peroxisome Proliferator-Activated Receptor Alpha Modulators (SPPARMα) in the Metabolic Syndrome: Is Pemafibrate Light at the End of the Tunnel? | Details |
| A05366 | 33281535 | Food Nutr Res | Bile salt hydrolase-overexpressing Lactobacillus strains can improve hepatic lipid accumulation in vitro in an NAFLD cell model. | Details |