DGIdb - PPARA Gene Record

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
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

(12 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
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.
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.
Guerre-Millo et al., 2000, Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity., J. Biol. Chem.
Clavey et al., 1999, Cell culture conditions determine apolipoprotein CIII secretion and regulation by fibrates in human hepatoma HepG2 cells., Cell. Physiol. Biochem.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Casas et al., 2000, New molecular aspects of regulation of mitochondrial activity by fenofibrate and fasting., FEBS Lett.
Chaput et al., 2000, Fenofibrate and rosiglitazone lower serum triglycerides with opposing effects on body weight., Biochem. Biophys. Res. Commun.
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
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
de Keyser CE et al., 2013, Genetic variation in the PPARA gene is associated with simvastatin-mediated cholesterol reduction in the Rotterdam Study., Pharmacogenomics
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
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
Giampietro L et al., 2012, Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs., Bioorg Med Chem Lett
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
Felts AS et al., 2008, Sulindac derivatives that activate the peroxisome proliferator-activated receptor gamma but lack cyclooxygenase inhibition., J Med Chem
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
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.
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
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.
Bonilla et al., 2001, Effect of a pharmacological activation of PPAR on the expression of RAR and TR in rat liver., J. Physiol. Biochem.
Guan et al., 2001, Peroxisome proliferator-activated receptors (PPARs): novel therapeutic targets in renal disease., Kidney Int.
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
Egerod FL et al., 2005, Biomarkers for early effects of carcinogenic dual-acting PPAR agonists in rat urinary bladder urothelium in vivo., Biomarkers
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.
Pahan et al., 2002, Gemfibrozil, a lipid-lowering drug, inhibits the induction of nitric-oxide synthase in human astrocytes., J. Biol. Chem.
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.
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
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
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
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
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.
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.
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.
Hunt et al., 2000, Involvement of the peroxisome proliferator-activated receptor alpha in regulating long-chain acyl-CoA thioesterases., J. Lipid Res.
Lancia P et al., 2018, Pharmacogenetics of post-transplant diabetes mellitus in children with renal transplantation treated with tacrolimus., Pediatr Nephrol
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
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
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
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
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
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
Cano C et al., 2007, Novel sulfamide analogs of oleoylethanolamide showing in vivo satiety inducing actions and PPARalpha activation., 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.
Botton MR et al., 2015, PPARA gene and phenprocoumon: a new predictor of response variability., Pharmacogenet Genomics

BEZAFIBRATE PPARA

Interaction Score: 5.8

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name CRx-401

Novel drug target Established target

Specific Action of the Ligand Agonist

PMIDs:
10933891 10909982 18629356 16511610 11172467 11519881 11422732 11752352

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
LY-518674 PPARA

Interaction Score: 3.87

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 ChemblInteractions GuideToPharmacology TTD
MYRISTIC ACID PPARA

Interaction Score: 1.93

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10403814

Sources:
DTC
GW590735 PPARA

Interaction Score: 1.93

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
10592235

Sources:
ChemblInteractions
ROMAZARIT PPARA

Interaction Score: 1.93

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23515070

Sources:
TTD
CHEMBL107518 PPARA

Interaction Score: 1.93

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22487179

Sources:
DTC
ALEGLITAZAR PPARA

Interaction Score: 1.93

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

Trial Name aleglitazar, R1439

PMIDs:
10592235 20653327

Sources:
TdgClinicalTrial ChemblInteractions
RAGAGLITAZAR PPARA

Interaction Score: 1.93

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

PMIDs:
16240504 12970088

Sources:
GuideToPharmacology TTD
CHEMBL1089501 PPARA

Interaction Score: 1.93

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20218621

Sources:
DTC
K-877 PPARA

Interaction Score: 1.93

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

PMIDs:
None found

Sources:
ChemblInteractions TTD
FENOFIBRIC ACID PPARA

Interaction Score: 1.61

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
23566516 21855333 22579484

Sources:
DTC ChemblInteractions
TESAGLITAZAR PPARA

Interaction Score: 1.45

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
16168052

Sources:
ChemblInteractions TTD
NAVEGLITAZAR PPARA

Interaction Score: 1.45

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 ChemblInteractions TTD
IMIGLITAZAR PPARA

Interaction Score: 1.45

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:
ChemblInteractions GuideToPharmacology TTD
GW501516 PPARA

Interaction Score: 1.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name GW501516

Novel drug target Established target

PMIDs:
23566516 23843199

Sources:
DTC TdgClinicalTrial
CIPROFIBRATE PPARA

Interaction Score: 1.29

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 GuideToPharmacology TTD
DRF-10945 PPARA

Interaction Score: 0.97

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHOLINE FENOFIBRATE PPARA

Interaction Score: 0.97

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: 0.97

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17228882 26071639

Sources:
DTC
CHEMBL270960 PPARA

Interaction Score: 0.97

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: 0.97

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: 0.97

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: 0.97

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: 0.97

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: 0.89

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

Direct Interaction? True

PMIDs:
12244038 12834305 10494028 12172398 12935323 21889235

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
PIRINIXIC ACID PPARA

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25497132 23171045 17228882

Sources:
DTC
CLOFIBRATE PPARA

Interaction Score: 0.71

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
10922459 20637823 10951268 20671072 10753628 10454501 10787442

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
INDEGLITAZAR PPARA

Interaction Score: 0.64

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor agonist

Direct Interaction yes

PMIDs:
10592235

Sources:
ChemblInteractions
PROSTAGLANDIN D2 PPARA

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23566516

Sources:
DTC
LXR-623 PPARA

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20350005

Sources:
DTC
LY-510929 PPARA

Interaction Score: 0.48

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
REGLITAZAR PPARA

Interaction Score: 0.48

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: 0.48

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
MURAGLITAZAR PPARA

Interaction Score: 0.48

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 ChemblInteractions TTD
LACTOFEN PPARA

Interaction Score: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ELAFIBRANOR PPARA

Interaction Score: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
OXEGLITAZAR PPARA

Interaction Score: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
LOBEGLITAZONE PPARA

Interaction Score: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHEMBL410478 PPARA

Interaction Score: 0.48

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: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MK-0767 PPARA

Interaction Score: 0.48

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: 0.47

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:
11474486 11342537 10828060 10494028 11752352 11018525 10799317 15608561

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD
CHEMBL220087 PPARA

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CIGLITAZONE PPARA

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23566516

Sources:
DTC
SODELGLITAZAR PPARA

Interaction Score: 0.32

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: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
FARGLITAZAR PPARA

Interaction Score: 0.32

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: 0.32

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: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PHENPROCOUMON PPARA

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25461249

Sources:
PharmGKB
BROMOXYNIL PPARA

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PHENFORMIN HYDROCHLORIDE PPARA

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TETRADECYLTHIOACETIC ACID PPARA

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20036122

Sources:
DTC
CHEMBL118417 PPARA

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GW7647 PPARA

Interaction Score: 0.2

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
23171045 23102891 18162399 18665581

Sources:
DTC GuideToPharmacology
LINOLEIC ACID PPARA

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
URSOLIC ACID PPARA

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21855333

Sources:
DTC
CHEMBL153057 PPARA

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
T091317 PPARA

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20350005

Sources:
DTC
CHEMBL38508 PPARA

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
OLEIC ACID PPARA

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TACROLIMUS PPARA

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29399716 24658827 24113216

Sources:
PharmGKB
ILOPROST PPARA

Interaction Score: 0.11

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC
SIMVASTATIN PPARA

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24598718 23930676 23252946

Sources:
PharmGKB
METFORMIN PPARA

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24853734

Sources:
PharmGKB
BITHIONOL PPARA

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

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

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:
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:
GO: PPARA
- Version: 01-May-2021
Alternate Names:

NR1C1 GO Gene Synonym

PPAR GO Gene Synonym

Gene Info:

Gene Categories:

TRANSCRIPTION FACTOR BINDING, NUCLEAR HORMONE RECEPTOR

Publications:
Pharos: PPARA
- Version: 01-May-2021
Alternate Names:

Peroxisome proliferator-activated receptor alpha Gene Name

Q07869 UniProt ID

Gene Info:

Gene Categories:

ENZYME, TRANSCRIPTION FACTOR

Publications:

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

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

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

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

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

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

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

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

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

5465	Entrez Gene Id
PPARA_HUMAN	Uniprot Id
ENSG00000186951	Ensembl Gene Id

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

9232	HUGO Gene ID
9232	HUGO Gene Symbol
peroxisome proliferator activated receptor alpha	HUGO Gene Name

PPAR	GENE_SYMBOL
PPARA	GENE_SYMBOL
Peroxisome proliferator-activated receptor alpha	UNIPROT

Peroxisome proliferator-activated receptor alpha	Gene Name
Q07869	UniProt ID

PPARA Gene Record

PPARA 5465 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 10933891 10909982 18629356 16511610 11172467 11519881 11422732 11752352

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

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 ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10403814

Sources: DTC

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 10592235

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23515070

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22487179

Sources: DTC

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 10592235 20653327

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 16240504 12970088

Sources: GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20218621

Sources: DTC

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 23566516 21855333 22579484

Sources: DTC ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 16168052

Sources: ChemblInteractions TTD

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 ChemblInteractions TTD

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: ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name GW501516 Novel drug target Established target

PMIDs: 23566516 23843199

Sources: DTC TdgClinicalTrial

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 16731579

Sources: DTC GuideToPharmacology TTD

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name CRx-401

Novel drug target Established target

Specific Action of the Ligand Agonist

PMIDs:
10933891 10909982 18629356 16511610 11172467 11519881 11422732 11752352

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

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 ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
10403814

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
10592235

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
23515070

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
22487179

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

Trial Name aleglitazar, R1439

PMIDs:
10592235 20653327

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

PMIDs:
16240504 12970088

Sources:
GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
20218621

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
23566516 21855333 22579484

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
16168052

Sources:
ChemblInteractions TTD

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 ChemblInteractions TTD

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:
ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name GW501516

Novel drug target Established target

PMIDs:
23566516 23843199

Sources:
DTC TdgClinicalTrial

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 GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
17228882 26071639

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)