Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTK095PP)

DOT Name Peroxisome proliferator-activated receptor alpha (PPARA)
Synonyms PPAR-alpha; Nuclear receptor subfamily 1 group C member 1
Gene Name PPARA
UniProt ID
PPARA_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
1I7G ; 1K7L ; 1KKQ ; 2NPA ; 2P54 ; 2REW ; 2ZNN ; 3ET1 ; 3FEI ; 3G8I ; 3KDT ; 3KDU ; 3SP6 ; 3VI8 ; 4BCR ; 4CI4 ; 5AZT ; 5HYK ; 6KAX ; 6KAY ; 6KAZ ; 6KB0 ; 6KB1 ; 6KB2 ; 6KB3 ; 6KB4 ; 6KB5 ; 6KB6 ; 6KB7 ; 6KB8 ; 6KB9 ; 6KBA ; 6KXX ; 6KXY ; 6KYP ; 6L36 ; 6L37 ; 6L38 ; 6L96 ; 6LX4 ; 6LX5 ; 6LX6 ; 6LX7 ; 6LX8 ; 6LX9 ; 6LXA ; 6LXB ; 6LXC ; 7BPY ; 7BPZ ; 7BQ0 ; 7BQ1 ; 7BQ2 ; 7BQ3 ; 7BQ4 ; 7C6Q ; 7E5F ; 7E5G ; 7E5H ; 7E5I ; 8HUK ; 8HUN ; 8HUQ
Pfam ID
PF00104 ; PF00105
Sequence
MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSC
PGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACE
GCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSE
KAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFV
IHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANL
DLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFD
FAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDI
FLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY
Function
Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety. Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as a transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2. May be required for the propagation of clock information to metabolic pathways regulated by PER2.
Tissue Specificity Skeletal muscle, liver, heart and kidney. Expressed in monocytes .
KEGG Pathway
PPAR sig.ling pathway (hsa03320 )
cAMP sig.ling pathway (hsa04024 )
Adipocytokine sig.ling pathway (hsa04920 )
Glucagon sig.ling pathway (hsa04922 )
Insulin resistance (hsa04931 )
Non-alcoholic fatty liver disease (hsa04932 )
Alcoholic liver disease (hsa04936 )
Hepatitis C (hsa05160 )
Chemical carcinogenesis - receptor activation (hsa05207 )
Diabetic cardiomyopathy (hsa05415 )
Reactome Pathway
BMAL1 (R-HSA-1368108 )
PPARA activates gene expression (R-HSA-1989781 )
Transcriptional activation of mitochondrial biogenesis (R-HSA-2151201 )
Activation of gene expression by SREBF (SREBP) (R-HSA-2426168 )
Transcriptional regulation of white adipocyte differentiation (R-HSA-381340 )
Nuclear Receptor transcription pathway (R-HSA-383280 )
Regulation of lipid metabolism by PPARalpha (R-HSA-400206 )
Circadian Clock (R-HSA-400253 )
SUMOylation of intracellular receptors (R-HSA-4090294 )
Cytoprotection by HMOX1 (R-HSA-9707564 )
Heme signaling (R-HSA-9707616 )
RORA activates gene expression (R-HSA-1368082 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 1 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Tacrolimus DMZ7XNQ Approved Peroxisome proliferator-activated receptor alpha (PPARA) affects the response to substance of Tacrolimus. [64]
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6 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the methylation of Peroxisome proliferator-activated receptor alpha (PPARA). [1]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the methylation of Peroxisome proliferator-activated receptor alpha (PPARA). [39]
Taxifolin DMQJSF9 Preclinical Taxifolin increases the phosphorylation of Peroxisome proliferator-activated receptor alpha (PPARA). [43]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the methylation of Peroxisome proliferator-activated receptor alpha (PPARA). [44]
schisandrin A DMWQ480 Investigative schisandrin A increases the phosphorylation of Peroxisome proliferator-activated receptor alpha (PPARA). [43]
Phthalic Acid DMF9T64 Investigative Phthalic Acid decreases the methylation of Peroxisome proliferator-activated receptor alpha (PPARA). [44]
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⏷ Show the Full List of 6 Drug(s)
68 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [2]
Tretinoin DM49DUI Approved Tretinoin increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [3]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [4]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [5]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [6]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [7]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [8]
Ivermectin DMDBX5F Approved Ivermectin decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [9]
Arsenic DMTL2Y1 Approved Arsenic decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [10]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [11]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [12]
Testosterone DM7HUNW Approved Testosterone increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [13]
Triclosan DMZUR4N Approved Triclosan decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [14]
Methotrexate DM2TEOL Approved Methotrexate increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [15]
Marinol DM70IK5 Approved Marinol increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [16]
Zoledronate DMIXC7G Approved Zoledronate decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [17]
Phenobarbital DMXZOCG Approved Phenobarbital increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [18]
Troglitazone DM3VFPD Approved Troglitazone increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [19]
Ethanol DMDRQZU Approved Ethanol decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [21]
Aspirin DM672AH Approved Aspirin increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [22]
Indomethacin DMSC4A7 Approved Indomethacin increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [23]
Capsaicin DMGMF6V Approved Capsaicin decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [24]
Pioglitazone DMKJ485 Approved Pioglitazone increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [19]
Eicosapentaenoic acid/docosa-hexaenoic acid DMMUCG4 Approved Eicosapentaenoic acid/docosa-hexaenoic acid increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [19]
Clofibrate DMPC1J7 Approved Clofibrate increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [25]
Prasterone DM67VKL Approved Prasterone increases the activity of Peroxisome proliferator-activated receptor alpha (PPARA). [26]
Vitamin B3 DMQVRZH Approved Vitamin B3 increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [27]
Allopurinol DMLPAOB Approved Allopurinol increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [28]
Gemfibrozil DMD8Q3J Approved Gemfibrozil increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [29]
Pitavastatin DMJH792 Approved Pitavastatin increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [30]
Urea DMUK75B Approved Urea increases the activity of Peroxisome proliferator-activated receptor alpha (PPARA). [31]
Urethane DM7NSI0 Phase 4 Urethane decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [32]
SNDX-275 DMH7W9X Phase 3 SNDX-275 increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [33]
Resveratrol DM3RWXL Phase 3 Resveratrol increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [34]
Atorvastatin DMF28YC Phase 3 Trial Atorvastatin decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [30]
EXISULIND DMBY56U Phase 3 EXISULIND increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [35]
Tocopherol DMBIJZ6 Phase 2 Tocopherol increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [36]
GSK2110183 DMZHB37 Phase 2 GSK2110183 increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [37]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [40]
PMID26394986-Compound-22 DM43Z1G Patented PMID26394986-Compound-22 increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [23]
GW-501516 DMPL2KM Discontinued in Phase 4 GW-501516 increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [29]
MK-886 DMT0O7H Discontinued in Phase 2 MK-886 increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [41]
Ciglitazone DMAPO0T Preclinical Ciglitazone increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [42]
Nimesulide DMR1NMD Terminated Nimesulide decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [42]
NS398 DMINUWH Terminated NS398 decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [42]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [45]
Hexadecanoic acid DMWUXDZ Investigative Hexadecanoic acid decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [46]
D-glucose DMMG2TO Investigative D-glucose decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [47]
geraniol DMS3CBD Investigative geraniol increases the activity of Peroxisome proliferator-activated receptor alpha (PPARA). [48]
2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE DMNQL17 Investigative 2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [49]
Arachidonic acid DMUOQZD Investigative Arachidonic acid increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [19]
U0126 DM31OGF Investigative U0126 increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [50]
Dibutyl phthalate DMEDGKO Investigative Dibutyl phthalate increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [51]
Chrysin DM7V2LG Investigative Chrysin decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [52]
OXYBENZONE DMMZYX6 Investigative OXYBENZONE increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [53]
Linalool DMGZQ5P Investigative Linalool increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [54]
Oleic acid DM54O1Z Investigative Oleic acid decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [55]
Linoleic acid DMDGPY9 Investigative Linoleic acid increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [19]
MANGIFERIN DMWAF5Z Investigative MANGIFERIN increases the activity of Peroxisome proliferator-activated receptor alpha (PPARA). [56]
T0901317 DMZQVDI Investigative T0901317 increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [29]
Icosapentum DMF1CM7 Investigative Icosapentum increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [19]
OXYRESVERATROL DMN7S4L Investigative OXYRESVERATROL increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [57]
PAF DMRZAQW Investigative PAF decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [58]
Alpha-linolenic acid DMY64HE Investigative Alpha-linolenic acid increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [12]
pregnenolone-16alpha-carbonitrile DM0LW7G Investigative pregnenolone-16alpha-carbonitrile increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [18]
PHENYLTHIOUREA DMM1IAU Investigative PHENYLTHIOUREA increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [60]
Raffinose DMVHDOS Investigative Raffinose increases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [61]
XCT790 DMZ7N8D Investigative XCT790 decreases the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [62]
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⏷ Show the Full List of 68 Drug(s)
8 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
Rosiglitazone DMILWZR Approved Rosiglitazone affects the binding of Peroxisome proliferator-activated receptor alpha (PPARA). [20]
LTB4 DME26RS Phase 2 LTB4 affects the binding of Peroxisome proliferator-activated receptor alpha (PPARA). [38]
Fibrates DMFNTMY Investigative Fibrates affects the binding of Peroxisome proliferator-activated receptor alpha (PPARA). [20]
Caprylic acid DMLGS82 Investigative Caprylic acid affects the binding of Peroxisome proliferator-activated receptor alpha (PPARA). [59]
Lauric Acid DM9C8KQ Investigative Lauric Acid affects the binding of Peroxisome proliferator-activated receptor alpha (PPARA). [38]
L-165041 DMZP7YM Investigative L-165041 affects the binding of Peroxisome proliferator-activated receptor alpha (PPARA). [20]
MYRISTIC ACID DMYX0BL Investigative MYRISTIC ACID affects the binding of Peroxisome proliferator-activated receptor alpha (PPARA). [38]
Phytanic acid DMSZ1RB Investigative Phytanic acid affects the binding of Peroxisome proliferator-activated receptor alpha (PPARA). [63]
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⏷ Show the Full List of 8 Drug(s)

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