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PPARA Gene Record

  • Summary
  • Interactions
  • Claims
  • PPARA 5465 Druggable Genome

    Alternate Names:

    5465
    PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA
    PPARA
    NR1C1
    PPAR
    PPARalpha
    hPPAR
    170998
    9232
    ENSG00000186951
    OTTHUMG00000150443
    593
    Peroxisome proliferator-activated receptor-α
    peroxisome proliferator-activated receptor alpha
    NP_001001928
    NM_001001928
    Q07869
    PPAR-alpha
    Nuclear receptor subfamily 1 group C member 1
    PPARA_HUMAN
    BE0000071
    PA280
    PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA (PPAR-ALPHA). [SOURCE:UNIPROT/SWISSPROT;ACC:Q07869]
    T86591

    Gene Info:

    GuideToPharmacology Gene Category Name 1C. Peroxisome proliferator-activated receptors
    GuideToPharmacology Gene Category ID 86
    Target Class Receptors
    Target Subclass Nuclear receptor
    Target Main Class Receptors
    Human Readable Name NUCLEAR HORMONE RECEPTOR
    Uniprot Evidence 1: Evidence at protein level
    Human Readable Name DRUGGABLE GENOME
    Interpro Type Domain
    Interpro Acc IPR000536
    Uniprot Status Swiss-Prot
    Interpro Short Name Nucl_hrmn_rcpt_lig-bd_core
    Interpro Name Nuclear hormone receptor, ligand-binding, core
    Initial Gene Query NR1C1
    Counted Citations from 1950-2000 8485
    Gene Biotype PROTEIN_CODING
    (13 More Sources)

    Gene Categories: Category Details

    TRANSCRIPTION FACTOR BINDING
    NUCLEAR HORMONE RECEPTOR
    DRUGGABLE GENOME
    ENZYME
    TRANSCRIPTION FACTOR

    Publications:

    Hu B et al., 2010, Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist., J Med Chem
    Chaput et al., 2000, Fenofibrate and rosiglitazone lower serum triglycerides with opposing effects on body weight., Biochem. Biophys. Res. Commun.
    Casas et al., 2000, New molecular aspects of regulation of mitochondrial activity by fenofibrate and fasting., FEBS Lett.
    Guerre-Millo et al., 2000, Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity., J. Biol. Chem.
    Dana et al., 2001, Peroxisome proliferator-activated receptor subtype-specific regulation of hepatic and peripheral gene expression in the Zucker diabetic fatty rat., Metab. Clin. Exp.
    Clavey et al., 1999, Cell culture conditions determine apolipoprotein CIII secretion and regulation by fibrates in human hepatoma HepG2 cells., Cell. Physiol. Biochem.
    Bouly et al., 2001, Induction of the phospholipid transfer protein gene accounts for the high density lipoprotein enlargement in mice treated with fenofibrate., J. Biol. Chem.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Foucher C et al., 2004, Response to micronized fenofibrate treatment is associated with the peroxisome-proliferator-activated receptors alpha G/C intron7 polymorphism in subjects with type 2 diabetes., Pharmacogenetics
    de Keyser CE et al., 2013, Genetic variation in the PPARA gene is associated with simvastatin-mediated cholesterol reduction in the Rotterdam Study., Pharmacogenomics
    Tsamandouras N et al., 2014, Identification of the effect of multiple polymorphisms on the pharmacokinetics of simvastatin and simvastatin acid using a population-modeling approach., Clin Pharmacol Ther
    Hu M et al., 2013, Associations between the genotypes and phenotype of CYP3A and the lipid response to simvastatin in Chinese patients with hypercholesterolemia., Pharmacogenomics
    Giampietro L et al., 2012, Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs., Bioorg Med Chem Lett
    Felts AS et al., 2008, Sulindac derivatives that activate the peroxisome proliferator-activated receptor gamma but lack cyclooxygenase inhibition., J Med Chem
    Laghezza A et al., 2013, New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression., J Med Chem
    Kasuga J et al., 2008, SAR-oriented discovery of peroxisome proliferator-activated receptor pan agonist with a 4-adamantylphenyl group as a hydrophobic tail., Bioorg Med Chem Lett
    Li J et al., 2010, Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453)., J Med Chem
    Goldenberg et al., 2008, Update on the use of fibrates: focus on bezafibrate., Vasc Health Risk Manag
    Fruchart et al., 2006, Mode of action of fibrates in the regulation of triglyceride and HDL-cholesterol metabolism., Drugs Today
    Inoue et al., 2001, The ligands/activators for peroxisome proliferator-activated receptor alpha (PPARalpha) and PPARgamma increase Cu2+,Zn2+-superoxide dismutase and decrease p22phox message expressions in primary endothelial cells., Metab. Clin. Exp.
    Guan et al., 2001, Peroxisome proliferator-activated receptors (PPARs): novel therapeutic targets in renal disease., Kidney Int.
    Bonilla et al., 2001, Effect of a pharmacological activation of PPAR on the expression of RAR and TR in rat liver., J. Physiol. Biochem.
    Pedraza et al., 2000, Impaired expression of the uncoupling protein-3 gene in skeletal muscle during lactation: fibrates and troglitazone reverse lactation-induced downregulation of the uncoupling protein-3 gene., Diabetes
    Cabrero et al., 2000, Peroxisome proliferator-activated receptor alpha (PPARalpha) activators, bezafibrate and Wy-14,643, increase uncoupling protein-3 mRNA levels without modifying the mitochondrial membrane potential in primary culture of rat preadipocytes., Arch. Biochem. Biophys.
    Vanden Heuvel JP et al., 2006, Differential activation of nuclear receptors by perfluorinated fatty acid analogs and natural fatty acids: a comparison of human, mouse, and rat peroxisome proliferator-activated receptor-alpha, -beta, and -gamma, liver X receptor-beta, and retinoid X receptor-alpha., Toxicol Sci
    Chakrabarti et al., 2003, Ragaglitazar: a novel PPAR alpha PPAR gamma agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models., Br. J. Pharmacol.
    Egerod FL et al., 2005, Biomarkers for early effects of carcinogenic dual-acting PPAR agonists in rat urinary bladder urothelium in vivo., Biomarkers
    Pahan et al., 2002, Gemfibrozil, a lipid-lowering drug, inhibits the induction of nitric-oxide synthase in human astrocytes., J. Biol. Chem.
    Rizvi et al., 2003, Beneficial effects of fish liver preparations of sea bass (Lates calcarifer) versus gemfibrozil in high fat diet-induced lipid-intolerant rats., J Med Food
    Shoji et al., 2003, Preparation of antiserum against rat delta6-desaturase and its use to evaluate the desaturase protein levels in rats treated with gemfibrozil, a ligand for peroxisome proliferator-activated receptor alpha., Biosci. Biotechnol. Biochem.
    Bossé et al., Influences of the PPAR alpha-L162V polymorphism on plasma HDL(2)-cholesterol response of abdominally obese men treated with gemfibrozil., Genet. Med.
    De Filippis et al., 2011, Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism., Eur J Med Chem
    Cavender et al., 2010, Therapeutic potential of aleglitazar, a new dual PPAR-α/γ agonist: implications for cardiovascular disease in patients with diabetes mellitus., Am J Cardiovasc Drugs
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Hunt et al., 2000, Involvement of the peroxisome proliferator-activated receptor alpha in regulating long-chain acyl-CoA thioesterases., J. Lipid Res.
    Casas et al., 2000, A 45 kDa protein related to PPARgamma2, induced by peroxisome proliferators, is located in the mitochondrial matrix., FEBS Lett.
    Palkar et al., 2010, Effect of prenatal peroxisome proliferator-activated receptor alpha (PPARalpha) agonism on postnatal development., Toxicology
    Kömüves et al., 2000, Stimulation of PPARalpha promotes epidermal keratinocyte differentiation in vivo., J. Invest. Dermatol.
    Gelosa et al., 2010, Peroxisome proliferator-activated receptor {alpha} agonism prevents renal damage and the oxidative stress and inflammatory processes affecting the brains of stroke-prone rats., J. Pharmacol. Exp. Ther.
    Barclay et al., 1999, Modulation of cytochrome P-450 gene expression in endotoxemic mice is tissue specific and peroxisome proliferator-activated receptor-alpha dependent., J. Pharmacol. Exp. Ther.
    Murata et al., 2000, Stimulation by eicosapentaenoic acids of leptin mRNA expression and its secretion in mouse 3T3-L1 adipocytes in vitro., Biochem. Biophys. Res. Commun.
    Lunde I et al., 2014, The influence of CYP3A, PPARA, and POR genetic variants on the pharmacokinetics of tacrolimus and cyclosporine in renal transplant recipients., Eur J Clin Pharmacol
    Elens L et al., 2013, Single-nucleotide polymorphisms in P450 oxidoreductase and peroxisome proliferator-activated receptor-α are associated with the development of new-onset diabetes after transplantation in kidney transplant recipients treated with tacrolimus., Pharmacogenet Genomics
    Lancia P et al., 2018, Pharmacogenetics of post-transplant diabetes mellitus in children with renal transplantation treated with tacrolimus., Pediatr Nephrol
    Tamasi et al., 2008, Modulation of receptor phosphorylation contributes to activation of peroxisome proliferator activated receptor alpha by dehydroepiandrosterone and other peroxisome proliferators., Mol. Pharmacol.
    Kohalmy et al., 2007, Dehydroepiandrosterone induces human CYP2B6 through the constitutive androstane receptor., Drug Metab. Dispos.
    Jia Y et al., 2011, Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism., Bioorg Med Chem Lett
    Bhurruth-Alcor Y et al., 2010, Novel phospholipid analogues of pan-PPAR activator tetradecylthioacetic acid are more PPAR alpha selective., Bioorg Med Chem Lett
    Hoang MH et al., 2012, Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells., Bioorg Med Chem Lett
    Sato A et al., 2013, Synthesis and evaluation of 2,3-dinorprostaglandins: Dinor-PGD1 and 13-epi-dinor-PGD1 are peroxisome proliferator-activated receptor α/γ dual agonists., Bioorg Med Chem Lett
    Goswami S et al., 2014, Genetic variants in transcription factors are associated with the pharmacokinetics and pharmacodynamics of metformin., Clin Pharmacol Ther
    Sarath Josh MK et al., 2014, Phthalates efficiently bind to human peroxisome proliferator activated receptor and retinoid X receptor α, β, γ subtypes: an in silico approach., J Appl Toxicol
    Asano M et al., 2012, Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists., Bioorg Med Chem Lett
    Cano C et al., 2007, Novel sulfamide analogs of oleoylethanolamide showing in vivo satiety inducing actions and PPARalpha activation., J Med Chem
    Piemontese L et al., 2015, Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175., Eur J Med Chem
    Kajita D et al., 2015, Design and synthesis of silicon-containing fatty acid amide derivatives as novel peroxisome proliferator-activated receptor (PPAR) agonists., Bioorg Med Chem Lett
    Tenenbaum et al., 2005, Dual and pan-peroxisome proliferator-activated receptors (PPAR) co-agonism: the bezafibrate lessons., Cardiovasc Diabetol
    van Eekeren IC et al., 2013, Fibrates as therapy for osteoarthritis and rheumatoid arthritis? A systematic review., Ther Adv Musculoskelet Dis
    Murakami et al., 1999, Evidence for direct binding of fatty acids and eicosanoids to human peroxisome proliferators-activated receptor alpha., Biochem. Biophys. Res. Commun.
    Lehmann et al., 1997, Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs., J. Biol. Chem.
    Botton MR et al., 2015, PPARA gene and phenprocoumon: a new predictor of response variability., Pharmacogenet Genomics
    Konno H et al., 2013, Melinjo (Gnetum gnemon L.) Seed Extract Decreases Serum Uric Acid Levels in Nonobese Japanese Males: A Randomized Controlled Study., Evid Based Complement Alternat Med
    Urizar NL et al., 2002, A natural product that lowers cholesterol as an antagonist ligand for FXR., Science
    Drevon CA, 2005, Fatty acids and expression of adipokines., Biochim Biophys Acta
    Inoue et al., 2002, Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB., Biochem. Biophys. Res. Commun.
    Erbe DV et al., 2005, Ertiprotafib improves glycemic control and lowers lipids via multiple mechanisms., Mol Pharmacol
    Mezei O et al., 2003, Soy isoflavones exert antidiabetic and hypolipidemic effects through the PPAR pathways in obese Zucker rats and murine RAW 264.7 cells., J Nutr
    Szalowska E et al., 2014, Model steatogenic compounds (amiodarone, valproic acid, and tetracycline) alter lipid metabolism by different mechanisms in mouse liver slices., PLoS One
    McCarthy TC et al., 2004, Disruption of hepatic lipid homeostasis in mice after amiodarone treatment is associated with peroxisome proliferator-activated receptor-alpha target gene activation., J Pharmacol Exp Ther
    Rudkowska I et al., 2009, Omega-3 fatty acids regulate gene expression levels differently in subjects carrying the PPARalpha L162V polymorphism., Genes Nutr
    Liu M et al., 2014, PPARα-independent actions of omega-3 PUFAs contribute to their beneficial effects on adiposity and glucose homeostasis., Sci Rep
    Rodríguez-Cruz M et al., 2017, Nutrigenomics of ω-3 fatty acids: Regulators of the master transcription factors., Nutrition
    Downie MM et al., 2004, Peroxisome proliferator-activated receptor and farnesoid X receptor ligands differentially regulate sebaceous differentiation in human sebaceous gland organ cultures in vitro., Br J Dermatol
  • LY-518674   PPARA

    Interaction Score: 2.47

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name LY-674
    Novel drug target Established target
    Specific Action of the Ligand Agonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

  • RAGAGLITAZAR   PPARA

    Interaction Score: 1.54

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    12970088 16240504


    Sources:
    TTD DrugBank GuideToPharmacology

  • OCTANOIC ACID   PPARA

    Interaction Score: 1.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16731579


    Sources:
    DrugBank

  • ROMAZARIT   PPARA

    Interaction Score: 1.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23515070


    Sources:
    TTD

  • TESAGLITAZAR   PPARA

    Interaction Score: 1.23

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes

    PMIDs:
    16168052


    Sources:
    TTD DrugBank ChemblInteractions

  • CHEMBL107518   PPARA

    Interaction Score: 1.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22487179


    Sources:
    DTC

  • CHEMBL1089501   PPARA

    Interaction Score: 1.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20218621


    Sources:
    DTC

  • K-877   PPARA

    Interaction Score: 1.23

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • BEZAFIBRATE   PPARA

    Interaction Score: 1.15

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name CRx-401
    Novel drug target Established target
    Specific Action of the Ligand Agonist

    PMIDs:
    18629356 16511610 11172467 11422732 11519881 10909982 11752352 10933891


    Sources:
    TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • GW501516   PPARA

    Interaction Score: 1.03

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name GW501516
    Novel drug target Established target

    PMIDs:
    23566516 23843199


    Sources:
    DTC TdgClinicalTrial DrugBank

  • FENOFIBRIC ACID   PPARA

    Interaction Score: 1.03

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes

    PMIDs:
    22579484 21855333 23566516


    Sources:
    DTC ChemblInteractions

  • ALEGLITAZAR   PPARA

    Interaction Score: 1.03

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes
    Trial Name aleglitazar, R1439

    PMIDs:
    20653327 10592235


    Sources:
    TdgClinicalTrial DrugBank ChemblInteractions

  • CIPROFIBRATE   PPARA

    Interaction Score: 1.03

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Details of the Assay for Interaction Transactivation of a GAL4-PPARα ligand binding domain construct.
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    16731579


    Sources:
    DTC TTD DrugBank GuideToPharmacology

  • GW590735   PPARA

    Interaction Score: 0.93

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes

    PMIDs:
    10592235


    Sources:
    DrugBank ChemblInteractions

  • NAVEGLITAZAR   PPARA

    Interaction Score: 0.93

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name LY519818 , LY818
    Novel drug target Established target
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD ChemblInteractions

  • IMIGLITAZAR   PPARA

    Interaction Score: 0.93

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • DRF-10945   PPARA

    Interaction Score: 0.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • REGLITAZAR   PPARA

    Interaction Score: 0.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    DrugBank GuideToPharmacology

  • CHOLINE FENOFIBRATE   PPARA

    Interaction Score: 0.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • OLEOYLETHANOLAMIDE   PPARA

    Interaction Score: 0.62

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26071639 17228882


    Sources:
    DTC

  • CHEMBL270960   PPARA

    Interaction Score: 0.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ZYH7   PPARA

    Interaction Score: 0.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHEMBL500272   PPARA

    Interaction Score: 0.62

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CP-778875   PPARA

    Interaction Score: 0.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AVE8134   PPARA

    Interaction Score: 0.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • GEMFIBROZIL   PPARA

    Interaction Score: 0.57

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes
    Direct Interaction? True

    PMIDs:
    12244038 12935323 12834305 12172398 10494028 21889235


    Sources:
    TEND DTC TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • ELAIDIC ACID   PPARA

    Interaction Score: 0.49

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15491415 10403814 16731579


    Sources:
    DrugBank

  • PIRINIXIC ACID   PPARA

    Interaction Score: 0.49

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23171045 17228882 25497132


    Sources:
    DTC

  • CLOFIBRATE   PPARA

    Interaction Score: 0.49

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    10787442 10922459 20637823 10951268 20671072 10454501 10753628


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • INDEGLITAZAR   PPARA

    Interaction Score: 0.46

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor agonist
    Direct Interaction yes

    PMIDs:
    10592235


    Sources:
    DrugBank ChemblInteractions

  • LEUKOTRIENE_B4   PPARA

    Interaction Score: 0.41

    Interaction Types & Directionality:
    activator (activating)

    Interaction Info:

    PMIDs:
    15491415


    Sources:
    DrugBank

  • STEARIC ACID   PPARA

    Interaction Score: 0.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10403814


    Sources:
    DrugBank

  • CLINOFIBRATE   PPARA

    Interaction Score: 0.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11779144


    Sources:
    DrugBank

  • MYRRH   PPARA

    Interaction Score: 0.41

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    11988537


    Sources:
    DrugBank

  • MURAGLITAZAR   PPARA

    Interaction Score: 0.41

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name muraglitazar, BMS-298585
    Novel drug target Established target
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD DrugBank ChemblInteractions

  • ELAFIBRANOR   PPARA

    Interaction Score: 0.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD DrugBank

  • LXR-623   PPARA

    Interaction Score: 0.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20350005


    Sources:
    DTC

  • ERTIPROTAFIB   PPARA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15475571


    Sources:
    DrugBank

  • LY-510929   PPARA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • EDAGLITAZONE   PPARA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Details of the Assay for Interaction Measuring agonist-induced cofactor recruitment.
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • LACTOFEN   PPARA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • OXEGLITAZAR   PPARA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LOBEGLITAZONE   PPARA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CHEMBL410478   PPARA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL292352   PPARA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MK-0767   PPARA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Endogenous Drug? False
    Specific Action of the Ligand Agonist

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • FENOFIBRATE   PPARA

    Interaction Score: 0.3

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist
    Direct Interaction yes
    Trial Name ABT-335, choline fenofibrate,TriLipix

    PMIDs:
    10799317 11018525 10828060 11474486 10494028 11342537 11752352 15608561


    Sources:
    TEND PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

  • ISOFLAVONE   PPARA

    Interaction Score: 0.25

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    12730403


    Sources:
    DrugBank

  • FENOPROFEN   PPARA

    Interaction Score: 0.25

    Interaction Types & Directionality:
    activator (activating)

    Interaction Info:

    PMIDs:
    9013583


    Sources:
    DrugBank

  • PROSTAGLANDIN D2   PPARA

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23566516


    Sources:
    DTC

  • CHEMBL220087   PPARA

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CIGLITAZONE   PPARA

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23566516


    Sources:
    DTC

  • SODELGLITAZAR   PPARA

    Interaction Score: 0.21

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Peroxisome proliferator-activated receptor agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • IOXYNIL   PPARA

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • FARGLITAZAR   PPARA

    Interaction Score: 0.21

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • GSK-9578   PPARA

    Interaction Score: 0.21

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL259327   PPARA

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PHENPROCOUMON   PPARA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25461249


    Sources:
    PharmGKB

  • DOCONEXENT   PPARA

    Interaction Score: 0.17

    Interaction Types & Directionality:
    ligand

    Interaction Info:

    PMIDs:
    19585164 24986106


    Sources:
    DrugBank

  • BROMOXYNIL   PPARA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PHENFORMIN HYDROCHLORIDE   PPARA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TETRADECYLTHIOACETIC ACID   PPARA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20036122


    Sources:
    DTC

  • CHEMBL118417   PPARA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LUCINACTANT   PPARA

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10403814


    Sources:
    DrugBank

  • GW7647   PPARA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    23102891 18665581 23171045 18162399


    Sources:
    DTC GuideToPharmacology

  • PHTHALIC ACID   PPARA

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23843199


    Sources:
    DrugBank

  • FLUFENAMIC ACID   PPARA

    Interaction Score: 0.12

    Interaction Types & Directionality:
    activator (activating)

    Interaction Info:

    PMIDs:
    9013583


    Sources:
    DrugBank

  • FISH OIL TRIGLYCERIDES   PPARA

    Interaction Score: 0.12

    Interaction Types & Directionality:
    modulator

    Interaction Info:

    PMIDs:
    28760435


    Sources:
    DrugBank

  • ARACHIDONIC ACID   PPARA

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15491415 10403814


    Sources:
    DrugBank

  • DODECANOATE   PPARA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10403814


    Sources:
    DrugBank

  • ICOSAPENT   PPARA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10403814


    Sources:
    DrugBank

  • LINOLEIC ACID   PPARA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • URSOLIC ACID   PPARA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21855333


    Sources:
    DTC

  • CHEMBL153057   PPARA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DEXIBUPROFEN   PPARA

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9013583


    Sources:
    DrugBank

  • MYRISTIC ACID   PPARA

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10403814


    Sources:
    DTC DrugBank

  • CHEMBL38508   PPARA

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • OLEIC ACID   PPARA

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • T091317   PPARA

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20350005


    Sources:
    DTC

  • TACROLIMUS   PPARA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24658827 24113216 29399716


    Sources:
    PharmGKB

  • PRASTERONE   PPARA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    activator (activating)

    Interaction Info:

    PMIDs:
    18079279 17591676


    Sources:
    DrugBank

  • AMIODARONE   PPARA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    24489787 15265979


    Sources:
    DrugBank

  • LINOLENIC ACID   PPARA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10403814 16731579


    Sources:
    DrugBank

  • ROSIGLITAZONE   PPARA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15949695 11779144


    Sources:
    DrugBank

  • SIMVASTATIN   PPARA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23930676 24598718 23252946


    Sources:
    PharmGKB

  • ILOPROST   PPARA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    activator (activating)

    Interaction Info:
    Notes

    PMIDs:
    None found


    Sources:
    TALC

  • TROGLITAZONE   PPARA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11779144


    Sources:
    DrugBank

  • METFORMIN   PPARA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24853734


    Sources:
    PharmGKB

  • IBUPROFEN   PPARA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    activator (activating)

    Interaction Info:

    PMIDs:
    9013583


    Sources:
    DrugBank

  • INDOMETHACIN   PPARA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    9013583


    Sources:
    DrugBank

  • BITHIONOL   PPARA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RESVERATROL   PPARA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24454499


    Sources:
    DrugBank

  • Ensembl: ENSG00000186951

    • Version: 101_38

    Alternate Names:
    PPARA Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TdgClinicalTrial: Q07869

    • Version: January-2014

    Alternate Names:
    PPARA Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass Nuclear receptor

    Publications:

  • HopkinsGroom: Q07869

    • Version: 11-September-2012

    Alternate Names:
    5465 Entrez Gene Id
    PPARA_HUMAN Uniprot Id
    ENSG00000186951 Ensembl Gene Id

    Gene Info:
    Uniprot Evidence 1: Evidence at protein level
    Human Readable Name DRUGGABLE GENOME
    Interpro Type Domain

    Gene Categories:
    NUCLEAR HORMONE RECEPTOR, DRUGGABLE GENOME

    Publications:

  • TEND: Q07869

    • Version: 01-August-2011

    Alternate Names:
    PPARA_HUMAN Uniprot Id
    PPARA Gene Symbol
    5465 Entrez Gene Id

    Gene Info:
    Target Main Class Receptors
    Target Subclass Nuclear receptor

    Publications:

  • RussLampel: ENSG00000186951

    • Version: 26-July-2011

    Alternate Names:
    PPARA Display Id
    ENSG00000186951 Ensembl Gene Id
    PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA (PPAR-ALPHA). [SOURCE:UNIPROT/SWISSPROT;ACC:Q07869] Description

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • BaderLabGenes: PPARA

    • Version: February-2014

    Alternate Names:
    5465 Entrez Gene ID

    Gene Info:
    Initial Gene Query NR1C1
    Counted Citations from 1950-2000 8485

    Gene Categories:
    NUCLEAR HORMONE RECEPTOR

    Publications:

  • GuideToPharmacology: 5465

    • Version: 29-September-2020

    Alternate Names:
    9232 HUGO Gene ID
    9232 HUGO Gene Symbol
    peroxisome proliferator activated receptor alpha HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name 1C. Peroxisome proliferator-activated receptors
    GuideToPharmacology Gene Category ID 86

    Gene Categories:
    NUCLEAR HORMONE RECEPTOR

    Publications:

  • PharmGKB: PPARA

    • Version: 18-August-2020

    Alternate Names:
    PA280 PharmGKB ID

    Gene Info:

    Publications:
    de Keyser CE et al., 2013, Genetic variation in the PPARA gene is associated with simvastatin-mediated cholesterol reduction in the Rotterdam Study., Pharmacogenomics
    Tsamandouras N et al., 2014, Identification of the effect of multiple polymorphisms on the pharmacokinetics of simvastatin and simvastatin acid using a population-modeling approach., Clin Pharmacol Ther
    Hu M et al., 2013, Associations between the genotypes and phenotype of CYP3A and the lipid response to simvastatin in Chinese patients with hypercholesterolemia., Pharmacogenomics

  • DrugBank: BE0000071

    • Version: 5.1.7

    Alternate Names:
    PPARA DrugBank Gene Name
    Q07869 UniProt Accession
    5465 Entrez Gene Id

    Gene Info:

    Publications:
    Murakami et al., 1999, Evidence for direct binding of fatty acids and eicosanoids to human peroxisome proliferators-activated receptor alpha., Biochem. Biophys. Res. Commun.
    Inoue et al., 2002, Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB., Biochem. Biophys. Res. Commun.
    Szalowska E et al., 2014, Model steatogenic compounds (amiodarone, valproic acid, and tetracycline) alter lipid metabolism by different mechanisms in mouse liver slices., PLoS One

  • TTD: Peroxisome proliferator-activated receptor alpha

    • Version: 2020.06.01

    Alternate Names:
    PPARA TTD Gene Abbreviation
    T86591 TTD Target ID

    Gene Info:

    Publications:
    van Eekeren IC et al., 2013, Fibrates as therapy for osteoarthritis and rheumatoid arthritis? A systematic review., Ther Adv Musculoskelet Dis

  • DTC: PPARA

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Laghezza A et al., 2013, New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression., J Med Chem
    Cano C et al., 2007, Novel sulfamide analogs of oleoylethanolamide showing in vivo satiety inducing actions and PPARalpha activation., J Med Chem
    Piemontese L et al., 2015, Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175., Eur J Med Chem

  • HingoraniCasas: ENSG00000186951

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000186951 Gene Symbol
    PPARA Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TALC: PPAR

    • Version: 12-May-2016

    Alternate Names:
    PPAR Gene Symbol

    Gene Info:

    Publications:

  • ChemblInteractions: NR1C1

    • Version: chembl_23

    Alternate Names:
    PPAR GENE_SYMBOL
    PPARA GENE_SYMBOL
    Peroxisome proliferator-activated receptor alpha UNIPROT

    Gene Info:

    Publications:

  • Pharos: PPARA

    • Version: 03-September-2020

    Alternate Names:
    Peroxisome proliferator-activated receptor alpha Gene Name
    Q07869 UniProt ID

    Gene Info:

    Gene Categories:
    ENZYME, TRANSCRIPTION FACTOR

    Publications:

  • GO: PPARA

    • Version: 05-September-2020

    Alternate Names:
    NR1C1 GO Gene Synonym
    PPAR GO Gene Synonym

    Gene Info:

    Gene Categories:
    TRANSCRIPTION FACTOR BINDING, NUCLEAR HORMONE RECEPTOR

    Publications:

  • dGene: PPARA

    • Version: 27-Jun-2013

    Alternate Names:
    5465 Gene ID
    NR1C1 dGene Synonym
    PPAR dGene Synonym

    Gene Info:

    Gene Categories:
    NUCLEAR HORMONE RECEPTOR

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21