Details of Drug Off-Target (DOT)

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

DOT Name Peroxisome proliferator-activated receptor gamma (PPARG)
Synonyms PPAR-gamma; Nuclear receptor subfamily 1 group C member 3
Gene Name PPARG
Related Disease
PPARG-related familial partial lipodystrophy ( )
Berardinelli-Seip congenital lipodystrophy ( )
UniProt ID
PPARG_HUMAN
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
PDB ID
1FM6 ; 1FM9 ; 1I7I ; 1K74 ; 1KNU ; 1NYX ; 1PRG ; 1RDT ; 1WM0 ; 1ZEO ; 1ZGY ; 2ATH ; 2F4B ; 2FVJ ; 2G0G ; 2G0H ; 2GTK ; 2HFP ; 2HWQ ; 2HWR ; 2I4J ; 2I4P ; 2I4Z ; 2OM9 ; 2P4Y ; 2POB ; 2PRG ; 2Q59 ; 2Q5P ; 2Q5S ; 2Q61 ; 2Q6R ; 2Q6S ; 2Q8S ; 2QMV ; 2VSR ; 2VST ; 2VV0 ; 2VV1 ; 2VV2 ; 2VV3 ; 2VV4 ; 2XKW ; 2YFE ; 2ZK0 ; 2ZK1 ; 2ZK2 ; 2ZK3 ; 2ZK4 ; 2ZK5 ; 2ZK6 ; 2ZNO ; 2ZVT ; 3ADS ; 3ADT ; 3ADU ; 3ADV ; 3ADW ; 3ADX ; 3AN3 ; 3AN4 ; 3B0Q ; 3B0R ; 3B1M ; 3B3K ; 3BC5 ; 3CDP ; 3CDS ; 3CS8 ; 3CWD ; 3D6D ; 3DZU ; 3DZY ; 3E00 ; 3ET0 ; 3ET3 ; 3FEJ ; 3FUR ; 3G9E ; 3GBK ; 3H0A ; 3HO0 ; 3HOD ; 3IA6 ; 3K8S ; 3KMG ; 3LMP ; 3NOA ; 3OSI ; 3OSW ; 3PBA ; 3PO9 ; 3PRG ; 3QT0 ; 3R5N ; 3R8A ; 3R8I ; 3S9S ; 3SZ1 ; 3T03 ; 3TY0 ; 3U9Q ; 3V9T ; 3V9V ; 3V9Y ; 3VJH ; 3VJI ; 3VN2 ; 3VSO ; 3VSP ; 3WJ4 ; 3WJ5 ; 3WMH ; 3X1H ; 3X1I ; 4A4V ; 4A4W ; 4CI5 ; 4E4K ; 4E4Q ; 4EM9 ; 4EMA ; 4F9M ; 4FGY ; 4HEE ; 4JAZ ; 4JL4 ; 4L96 ; 4L98 ; 4O8F ; 4OJ4 ; 4PRG ; 4PVU ; 4PWL ; 4R06 ; 4R2U ; 4R6S ; 4XLD ; 4XTA ; 4XUH ; 4XUM ; 4Y29 ; 4YT1 ; 5AZV ; 5DSH ; 5DV3 ; 5DV6 ; 5DV8 ; 5DVC ; 5DWL ; 5F9B ; 5GTN ; 5GTO ; 5GTP ; 5HZC ; 5JI0 ; 5LSG ; 5TTO ; 5TWO ; 5U5L ; 5UGM ; 5WQX ; 5WR0 ; 5WR1 ; 5Y2O ; 5Y2T ; 5YCN ; 5YCP ; 5Z5S ; 5Z6S ; 6AD9 ; 6AN1 ; 6AUG ; 6AVI ; 6C1I ; 6C5Q ; 6C5T ; 6D3E ; 6D8X ; 6D94 ; 6DBH ; 6DCU ; 6DGL ; 6DGO ; 6DGP ; 6DGQ ; 6DGR ; 6DH9 ; 6DHA ; 6E5A ; 6ENQ ; 6F2L ; 6FZF ; 6FZG ; 6FZJ ; 6FZP ; 6FZY ; 6ICJ ; 6IJR ; 6IJS ; 6ILQ ; 6IZM ; 6IZN ; 6JEY ; 6JF0 ; 6JQ7 ; 6K0T ; 6KTM ; 6KTN ; 6L89 ; 6L8B ; 6MCZ ; 6MD0 ; 6MD1 ; 6MD2 ; 6MD4 ; 6MS7 ; 6O67 ; 6O68 ; 6ONI ; 6ONJ ; 6PDZ ; 6QJ5 ; 6T1S ; 6T1V ; 6T6B ; 6T9C ; 6TDC ; 6TSG ; 6VZL ; 6VZM ; 6VZN ; 6VZO ; 6Y3U ; 6ZLY ; 7A7H ; 7AHJ ; 7AWC ; 7AWD ; 7CXE ; 7CXF ; 7CXG ; 7CXH ; 7CXI ; 7CXJ ; 7CXK ; 7CXL ; 7E0A ; 7E2O ; 7EFQ ; 7JQG ; 7LOT ; 7P4E ; 7QB1 ; 7RLE ; 7SQA ; 7SQB ; 7WGO ; 7WGP ; 7WGQ ; 7WOX ; 8ADF ; 8AQM ; 8AQN ; 8ATY ; 8ATZ ; 8B8W ; 8B8X ; 8B8Y ; 8B8Z ; 8B90 ; 8B91 ; 8B92 ; 8B93 ; 8B94 ; 8B95 ; 8BF1 ; 8BF2 ; 8BFF ; 8C0C ; 8CPH ; 8CPI ; 8CPJ ; 8DK4 ; 8DKN ; 8DKV ; 8DSY ; 8DSZ ; 8HHP ; 8HHQ ; 8WFE
Pfam ID
PF00104 ; PF12577 ; PF00105
Sequence
MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF
DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT
QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC
RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR
ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE
QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS
LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII
LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL
LQVIKKTETDMSLHPLLQEIYKDLY
Function
Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes, such as acyl-CoA oxidase. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis. ARF6 acts as a key regulator of the tissue-specific adipocyte P2 (aP2) enhancer. Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated pro-inflammatory responses. Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of BMAL1 in the blood vessels; (Microbial infection) Upon treatment with M.tuberculosis or its lipoprotein LpqH, phosphorylation of MAPK p38 and IL-6 production are modulated, probably via this protein.
Tissue Specificity Highest expression in adipose tissue. Lower in skeletal muscle, spleen, heart and liver. Also detectable in placenta, lung and ovary.
KEGG Pathway
PPAR sig.ling pathway (hsa03320 )
Efferocytosis (hsa04148 )
AMPK sig.ling pathway (hsa04152 )
Longevity regulating pathway (hsa04211 )
Osteoclast differentiation (hsa04380 )
Thermogenesis (hsa04714 )
Non-alcoholic fatty liver disease (hsa04932 )
Huntington disease (hsa05016 )
Pathways in cancer (hsa05200 )
Transcriptio.l misregulation in cancer (hsa05202 )
Thyroid cancer (hsa05216 )
Lipid and atherosclerosis (hsa05417 )
Reactome Pathway
Transcriptional regulation of white adipocyte differentiation (R-HSA-381340 )
Nuclear Receptor transcription pathway (R-HSA-383280 )
SUMOylation of intracellular receptors (R-HSA-4090294 )
Regulation of PTEN gene transcription (R-HSA-8943724 )
MECP2 regulates transcription factors (R-HSA-9022707 )
PPARA activates gene expression (R-HSA-1989781 )

Molecular Interaction Atlas (MIA) of This DOT

2 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
PPARG-related familial partial lipodystrophy DISVYGXS Definitive Autosomal dominant [1]
Berardinelli-Seip congenital lipodystrophy DISKW75N Supportive Autosomal recessive [2]
------------------------------------------------------------------------------------
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Regulation of Drug Effects of 1 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Adenosine triphosphate DM79F6G Approved Peroxisome proliferator-activated receptor gamma (PPARG) decreases the abundance of Adenosine triphosphate. [83]
------------------------------------------------------------------------------------
1 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate decreases the methylation of Peroxisome proliferator-activated receptor gamma (PPARG). [3]
------------------------------------------------------------------------------------
97 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [4]
Tretinoin DM49DUI Approved Tretinoin increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [5]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [6]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [7]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [8]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [9]
Arsenic DMTL2Y1 Approved Arsenic decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [10]
Quercetin DM3NC4M Approved Quercetin increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [11]
Temozolomide DMKECZD Approved Temozolomide decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [12]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [13]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [14]
Testosterone DM7HUNW Approved Testosterone decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [9]
Triclosan DMZUR4N Approved Triclosan increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [15]
Carbamazepine DMZOLBI Approved Carbamazepine affects the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [16]
Decitabine DMQL8XJ Approved Decitabine increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [17]
Marinol DM70IK5 Approved Marinol increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [18]
Zoledronate DMIXC7G Approved Zoledronate affects the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [19]
Phenobarbital DMXZOCG Approved Phenobarbital affects the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [20]
Fluorouracil DMUM7HZ Approved Fluorouracil decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [21]
Dexamethasone DMMWZET Approved Dexamethasone increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [22]
Niclosamide DMJAGXQ Approved Niclosamide increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [23]
Cannabidiol DM0659E Approved Cannabidiol increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [24]
Troglitazone DM3VFPD Approved Troglitazone increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [25]
Rosiglitazone DMILWZR Approved Rosiglitazone decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [26]
Ethanol DMDRQZU Approved Ethanol decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [27]
Aspirin DM672AH Approved Aspirin increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [28]
Irinotecan DMP6SC2 Approved Irinotecan decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [26]
Diclofenac DMPIHLS Approved Diclofenac increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [29]
Indomethacin DMSC4A7 Approved Indomethacin increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [30]
Cidofovir DMA13GD Approved Cidofovir affects the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [19]
Fenofibrate DMFKXDY Approved Fenofibrate increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [31]
Ifosfamide DMCT3I8 Approved Ifosfamide affects the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [19]
Clodronate DM9Y6X7 Approved Clodronate affects the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [19]
Capsaicin DMGMF6V Approved Capsaicin decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [32]
Alitretinoin DMME8LH Approved Alitretinoin increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [33]
Ibuprofen DM8VCBE Approved Ibuprofen affects the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [19]
Daunorubicin DMQUSBT Approved Daunorubicin decreases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [34]
Pioglitazone DMKJ485 Approved Pioglitazone increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [35]
Ursodeoxycholic acid DMCUT21 Approved Ursodeoxycholic acid decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [36]
Adefovir dipivoxil DMMAWY1 Approved Adefovir dipivoxil affects the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [19]
Ritonavir DMU764S Approved Ritonavir increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [37]
Chenodiol DMQ8JIK Approved Chenodiol increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [38]
Cholecalciferol DMGU74E Approved Cholecalciferol affects the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [39]
Bosentan DMIOGBU Approved Bosentan decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [40]
Bezafibrate DMZDCS0 Approved Bezafibrate decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [42]
Melatonin DMKWFBT Approved Melatonin decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [43]
Glucosamine DM4ZLFD Approved Glucosamine increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [44]
Isoniazid DM5JVS3 Approved Isoniazid decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [45]
Orlistat DMRJSP8 Approved Orlistat increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [46]
Eicosapentaenoic acid/docosa-hexaenoic acid DMMUCG4 Approved Eicosapentaenoic acid/docosa-hexaenoic acid increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [47]
Ximelegatran DMU8ANS Approved Ximelegatran increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [48]
Hesperetin DMKER83 Approved Hesperetin decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [49]
Nevirapine DM6HX9B Approved Nevirapine increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [50]
Busulfan DMXYJ9C Approved Busulfan affects the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [51]
Vitamin B3 DMQVRZH Approved Vitamin B3 increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [52]
Efavirenz DMC0GSJ Approved Efavirenz decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [50]
Cilostazol DMZMSCT Approved Cilostazol increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [53]
Stavudine DM6DEK9 Approved Stavudine decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [54]
Gemfibrozil DMD8Q3J Approved Gemfibrozil increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [31]
Valsartan DMREUQ6 Approved Valsartan decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [55]
Niflumic acid DMJ3I1Q Approved Niflumic acid increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [56]
Flufenamic Acid DMC8VNH Approved Flufenamic Acid increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [57]
Idarubicin DMM0XGL Approved Idarubicin decreases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [34]
Azelaic Acid DMHVL0J Approved Azelaic Acid increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [59]
Oxaprozin DM9UB0P Approved Oxaprozin increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [29]
Dihydrotestosterone DM3S8XC Phase 4 Dihydrotestosterone decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [60]
Berberine DMC5Q8X Phase 4 Berberine decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [61]
Lacidipine DMQP5I3 Phase 4 Lacidipine increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [34]
Resveratrol DM3RWXL Phase 3 Resveratrol increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [62]
Epigallocatechin gallate DMCGWBJ Phase 3 Epigallocatechin gallate decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [63]
Curcumin DMQPH29 Phase 3 Curcumin decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [64]
Fenretinide DMRD5SP Phase 3 Fenretinide increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [65]
EXISULIND DMBY56U Phase 3 EXISULIND increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [66]
Guaiacol DMN4E7T Phase 3 Guaiacol decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [63]
Avastin+/-Tarceva DMA86FL Phase 3 Avastin+/-Tarceva increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [67]
Telmisartan DMS3GX2 Phase 3 Trial Telmisartan increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [68]
Dalcetrapib DMKNCVM Phase 3 Dalcetrapib increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [69]
Anacetrapib DMP2BFG Phase 3 Anacetrapib increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [69]
Manidipine DMJPGUA Phase 3 Manidipine decreases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [34]
Cilnidipine DM1975O Phase 3 Cilnidipine decreases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [34]
CS-038 DM67P0F Phase 3 CS-038 increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [70]
TESAGLITAZAR DMGRBN5 Phase 3 TESAGLITAZAR increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [71]
Genistein DM0JETC Phase 2/3 Genistein decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [63]
Amiodarone DMUTEX3 Phase 2/3 Trial Amiodarone decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [51]
Phenol DM1QSM3 Phase 2/3 Phenol increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [72]
Thymoquinone DMVDTR2 Phase 2/3 Thymoquinone increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [73]
Tocopherol DMBIJZ6 Phase 2 Tocopherol increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [74]
phorbol 12-myristate 13-acetate DMJWD62 Phase 2 phorbol 12-myristate 13-acetate increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [75]
Disulfiram DMCL2OK Phase 2 Trial Disulfiram affects the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [76]
Puerarin DMJIMXH Phase 2 Puerarin decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [63]
Netoglitazone DM8H7OA Phase 2 Netoglitazone increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [77]
Icaritin DMGHQ37 Phase 2 Icaritin increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [78]
Pyrethroids DM1794O Phase 2 Pyrethroids increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [79]
LY-518674 DMBM2I9 Phase 2 LY-518674 increases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [31]
Mitoglitazone DMIRPSA Phase 2 Mitoglitazone increases the activity of Peroxisome proliferator-activated receptor gamma (PPARG). [80]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [81]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Peroxisome proliferator-activated receptor gamma (PPARG). [82]
------------------------------------------------------------------------------------
⏷ Show the Full List of 97 Drug(s)
2 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
Lovastatin DM9OZWQ Approved Lovastatin affects the localization of Peroxisome proliferator-activated receptor gamma (PPARG). [41]
Thiazolidinedione DMC1NBW Approved Thiazolidinedione affects the binding of Peroxisome proliferator-activated receptor gamma (PPARG). [58]
------------------------------------------------------------------------------------

References

1 Classification of Genes: Standardized Clinical Validity Assessment of Gene-Disease Associations Aids Diagnostic Exome Analysis and Reclassifications. Hum Mutat. 2017 May;38(5):600-608. doi: 10.1002/humu.23183. Epub 2017 Feb 13.
2 Biallelic mutations at PPARG cause a congenital, generalized lipodystrophy similar to the Berardinelli-Seip syndrome. Eur J Med Genet. 2014 Sep;57(9):524-6. doi: 10.1016/j.ejmg.2014.06.006. Epub 2014 Jun 28.
3 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
4 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
5 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
6 Blood transcript immune signatures distinguish a subset of people with elevated serum ALT from others given acetaminophen. Clin Pharmacol Ther. 2016 Apr;99(4):432-41.
7 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
8 Aldo-keto reductase 1B10 promotes development of cisplatin resistance in gastrointestinal cancer cells through down-regulating peroxisome proliferator-activated receptor--dependent mechanism. Chem Biol Interact. 2016 Aug 25;256:142-53. doi: 10.1016/j.cbi.2016.07.008. Epub 2016 Jul 11.
9 Testosterone or 17{beta}-estradiol exposure reveals sex-specific effects on glucose and lipid metabolism in human myotubes. J Endocrinol. 2011 Aug;210(2):219-29. doi: 10.1530/JOE-10-0497. Epub 2011 Jun 1.
10 Arsenic inhibits the adipogenic differentiation of mesenchymal stem cells by down-regulating peroxisome proliferator-activated receptor gamma and CCAAT enhancer-binding proteins. Toxicol In Vitro. 2013 Feb;27(1):211-9. doi: 10.1016/j.tiv.2012.10.012. Epub 2012 Oct 26.
11 The effect of quercetin and kaempferol aglycones and glucuronides on peroxisome proliferator-activated receptor-gamma (PPAR-). Food Funct. 2015 Apr;6(4):1098-107. doi: 10.1039/c5fo00076a.
12 Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
13 Regulatory role of KEAP1 and NRF2 in PPAR expression and chemoresistance in human non-small-cell lung carcinoma cells. Free Radic Biol Med. 2012 Aug 15;53(4):758-68. doi: 10.1016/j.freeradbiomed.2012.05.041. Epub 2012 Jun 7.
14 Protective effects of myricitrin against osteoporosis via reducing reactive oxygen species and bone-resorbing cytokines. Toxicol Appl Pharmacol. 2014 Nov 1;280(3):550-60.
15 Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
16 Drug-induced endoplasmic reticulum and oxidative stress responses independently sensitize toward TNF-mediated hepatotoxicity. Toxicol Sci. 2014 Jul;140(1):144-59. doi: 10.1093/toxsci/kfu072. Epub 2014 Apr 20.
17 Regulation of myofibroblast transdifferentiation by DNA methylation and MeCP2: implications for wound healing and fibrogenesis. Cell Death Differ. 2007 Feb;14(2):275-85. doi: 10.1038/sj.cdd.4401979. Epub 2006 Jun 9.
18 Tetrahydrocannabinolic acid is a potent PPAR agonist with neuroprotective activity. Br J Pharmacol. 2017 Dec;174(23):4263-4276. doi: 10.1111/bph.14019. Epub 2017 Nov 2.
19 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
20 Reproducible chemical-induced changes in gene expression profiles in human hepatoma HepaRG cells under various experimental conditions. Toxicol In Vitro. 2009 Apr;23(3):466-75. doi: 10.1016/j.tiv.2008.12.018. Epub 2008 Dec 30.
21 Dissecting progressive stages of 5-fluorouracil resistance in vitro using RNA expression profiling. Int J Cancer. 2004 Nov 1;112(2):200-12. doi: 10.1002/ijc.20401.
22 Theophylline and dexamethasone induce peroxisome proliferator-activated receptor-gamma expression in human eosinophils. Pharmacology. 2006;77(1):33-7. doi: 10.1159/000092376. Epub 2006 Mar 29.
23 Mitochondrial Uncoupling Induces Epigenome Remodeling and Promotes Differentiation in Neuroblastoma. Cancer Res. 2023 Jan 18;83(2):181-194. doi: 10.1158/0008-5472.CAN-22-1029.
24 COX-2 and PPAR-gama confer cannabidiol-induced apoptosis of human lung cancer cells. Mol Cancer Ther. 2013 Jan;12(1):69-82.
25 Induction of solid tumor differentiation by the peroxisome proliferator-activated receptor-gamma ligand troglitazone in patients with liposarcoma. Proc Natl Acad Sci U S A. 1999 Mar 30;96(7):3951-6. doi: 10.1073/pnas.96.7.3951.
26 The PPAR-dependent effect of flavonoid luteolin against damage induced by the chemotherapeutic irinotecan in human intestinal cells. Chem Biol Interact. 2022 Jan 5;351:109712. doi: 10.1016/j.cbi.2021.109712. Epub 2021 Oct 23.
27 NFATc4 mediates ethanol-triggered hepatocyte senescence. Toxicol Lett. 2021 Oct 10;350:10-21. doi: 10.1016/j.toxlet.2021.06.018. Epub 2021 Jun 27.
28 Aspirin inhibits MMP-9 mRNA expression and release via the PPARalpha/gamma and COX-2/mPGES-1-mediated pathways in macrophages derived from THP-1 cells. Biomed Pharmacother. 2010 Feb;64(2):118-23. doi: 10.1016/j.biopha.2009.04.033. Epub 2009 Oct 17.
29 Nonsteroidal anti-inflammatory drugs induce apoptosis in association with activation of peroxisome proliferator-activated receptor gamma in rheumatoid synovial cells. J Pharmacol Exp Ther. 2002 Jul;302(1):18-25. doi: 10.1124/jpet.302.1.18.
30 Induction of apoptosis in rheumatoid synovial fibroblasts by celecoxib, but not by other selective cyclooxygenase 2 inhibitors. Arthritis Rheum. 2002 Dec;46(12):3159-67. doi: 10.1002/art.10692.
31 On the mechanism for PPAR agonists to enhance ABCA1 gene expression. Atherosclerosis. 2009 Aug;205(2):413-9. doi: 10.1016/j.atherosclerosis.2009.01.008. Epub 2009 Jan 19.
32 Transient receptor potential vanilloid-1 signaling as a regulator of human sebocyte biology. J Invest Dermatol. 2009 Feb;129(2):329-39. doi: 10.1038/jid.2008.258. Epub 2008 Sep 4.
33 Proteasome inhibitors induce peroxisome proliferator-activated receptor transactivation through RXR accumulation and a protein kinase C-dependent pathway. Exp Cell Res. 2005 Mar 10;304(1):234-43. doi: 10.1016/j.yexcr.2004.11.004. Epub 2004 Dec 10.
34 Quantitative high-throughput profiling of environmental chemicals and drugs that modulate farnesoid X receptor. Sci Rep. 2014 Sep 26;4:6437. doi: 10.1038/srep06437.
35 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. Metabolism. 2001 Jan;50(1):3-11.
36 Ursodeoxycholic acid but not tauroursodeoxycholic acid inhibits proliferation and differentiation of human subcutaneous adipocytes. PLoS One. 2013 Dec 3;8(12):e82086. doi: 10.1371/journal.pone.0082086. eCollection 2013.
37 Estrogen prevents cholesteryl ester accumulation in macrophages induced by the HIV protease inhibitor ritonavir. J Cell Biochem. 2008 Apr 1;103(5):1598-606. doi: 10.1002/jcb.21546.
38 Chenodeoxycholic acid significantly impacts the expression of miRNAs and genes involved in lipid, bile acid and drug metabolism in human hepatocytes. Life Sci. 2016 Jul 1;156:47-56.
39 Targeting iron homeostasis induces cellular differentiation and synergizes with differentiating agents in acute myeloid leukemia. J Exp Med. 2010 Apr 12;207(4):731-50. doi: 10.1084/jem.20091488. Epub 2010 Apr 5.
40 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
41 Lovastatin lactone elicits human lung cancer cell apoptosis via a COX-2/PPAR-dependent pathway. Oncotarget. 2016 Mar 1;7(9):10345-62. doi: 10.18632/oncotarget.7213.
42 Expression of cFABP and PPAR in trophoblast cells: effect of PPAR ligands on linoleic acid uptake and differentiation. Biochim Biophys Acta. 2005 Feb 21;1687(1-3):181-94. doi: 10.1016/j.bbalip.2004.11.017.
43 Melatonin inhibits adipogenesis and enhances osteogenesis of human mesenchymal stem cells by suppressing PPAR expression and enhancing Runx2 expression. J Pineal Res. 2010 Nov;49(4):364-72. doi: 10.1111/j.1600-079X.2010.00803.x. Epub 2010 Aug 24.
44 Glucosamine sulfate reduces prostaglandin E(2) production in osteoarthritic chondrocytes through inhibition of microsomal PGE synthase-1. J Rheumatol. 2012 Mar;39(3):635-44. doi: 10.3899/jrheum.110621. Epub 2011 Nov 15.
45 Isoniazid suppresses antioxidant response element activities and impairs adipogenesis in mouse and human preadipocytes. Toxicol Appl Pharmacol. 2013 Dec 15;273(3):435-41. doi: 10.1016/j.taap.2013.10.005. Epub 2013 Oct 12.
46 Diosgenin and 4-Hydroxyisoleucine from Fenugreek Are Regulators of Genes Involved in Lipid Metabolism in The Human Colorectal Cancer Cell Line SW480. Cell J. 2021 Jan;22(4):514-522. doi: 10.22074/cellj.2021.6751. Epub 2020 Apr 22.
47 EPA and DHA reduce LPS-induced inflammation responses in HK-2 cells: evidence for a PPAR-gamma-dependent mechanism. Kidney Int. 2005 Mar;67(3):867-74. doi: 10.1111/j.1523-1755.2005.00151.x.
48 Effects of Y-27632 on the osteogenic and adipogenic potential of human dental pulp stem cells in vitro. Hum Exp Toxicol. 2022 Jan-Dec;41:9603271221089003. doi: 10.1177/09603271221089003.
49 Hesperetin inhibit adipocyte differentiation and enhance Bax- and p21-mediated adipolysis in human mesenchymal stem cell adipogenesis. J Biochem Mol Toxicol. 2015 Mar;29(3):99-108. doi: 10.1002/jbt.21672. Epub 2014 Oct 26.
50 Effects of nevirapine and efavirenz on human adipocyte differentiation, gene expression, and release of adipokines and cytokines. Antiviral Res. 2011 Aug;91(2):112-9. doi: 10.1016/j.antiviral.2011.04.018. Epub 2011 May 17.
51 Direct transcriptomic comparison of xenobiotic metabolism and toxicity pathway induction of airway epithelium models at an air-liquid interface generated from induced pluripotent stem cells and primary bronchial epithelial cells. Cell Biol Toxicol. 2023 Feb;39(1):1-18. doi: 10.1007/s10565-022-09726-0. Epub 2022 May 31.
52 Stimulation of CD36 and the key effector of reverse cholesterol transport ATP-binding cassette A1 in monocytoid cells by niacin. Biochem Pharmacol. 2004 Feb 1;67(3):411-9. doi: 10.1016/j.bcp.2003.09.014.
53 HO-1 Induced by Cilostazol Protects Against TNF--associated Cytotoxicity via a PPAR--dependent Pathway in Human Endothelial Cells. Korean J Physiol Pharmacol. 2011 Apr;15(2):83-8. doi: 10.4196/kjpp.2011.15.2.83. Epub 2011 Apr 30.
54 Mitochondrial proliferation, DNA depletion and adipocyte differentiation in subcutaneous adipose tissue of HIV-positive HAART recipients. Antivir Ther. 2003 Aug;8(4):323-31.
55 Valsartan improves adipose tissue function in humans with impaired glucose metabolism: a randomized placebo-controlled double-blind trial. PLoS One. 2012;7(6):e39930. doi: 10.1371/journal.pone.0039930. Epub 2012 Jun 29.
56 Combined treatment with the Cox-2 inhibitor niflumic acid and PPARgama ligand ciglitazone induces ER stress/caspase-8-mediated apoptosis in human lung cancer cells. Cancer Lett. 2011 Jan 28;300(2):134-44.
57 Two opposing effects of non-steroidal anti-inflammatory drugs on the expression of the inducible cyclooxygenaseMediation through different signaling pathways. J Biol Chem. 2000 Sep 8;275(36):28173-9.
58 Peroxisome proliferator-activated receptor gamma ligands induce cell cycle arrest and apoptosis in human renal carcinoma cell lines. Acta Pharmacol Sin. 2005 Jun;26(6):753-61. doi: 10.1111/j.1745-7254.2005.00753.x.
59 Azelaic acid modulates the inflammatory response in normal human keratinocytes through PPARgamma activation. Exp Dermatol. 2010 Sep;19(9):813-20. doi: 10.1111/j.1600-0625.2010.01107.x. Epub 2010 Jul 2.
60 Effects of dihydrotestosterone on differentiation and proliferation of human mesenchymal stem cells and preadipocytes. Mol Cell Endocrinol. 2008 Dec 16;296(1-2):32-40. doi: 10.1016/j.mce.2008.08.019. Epub 2008 Aug 28.
61 Berberine promotes bone marrow-derived mesenchymal stem cells osteogenic differentiation via canonical Wnt/-catenin signaling pathway. Toxicol Lett. 2016 Jan 5;240(1):68-80. doi: 10.1016/j.toxlet.2015.10.007. Epub 2015 Oct 22.
62 Novel PPAR pan agonist, ZBH ameliorates hyperlipidemia and insulin resistance in high fat diet induced hyperlipidemic hamster. PLoS One. 2014 Apr 23;9(4):e96056. doi: 10.1371/journal.pone.0096056. eCollection 2014.
63 Examining the genomic influence of skin antioxidants in vitro. Mediators Inflamm. 2010;2010.
64 Activation of PPAR{gamma} by curcumin inhibits Moser cell growth and mediates suppression of gene expression of cyclin D1 and EGFR. Am J Physiol Gastrointest Liver Physiol. 2005 Mar;288(3):G447-56. doi: 10.1152/ajpgi.00209.2004. Epub 2004 Oct 14.
65 PPAR activation and decreased proliferation in oral carcinoma cells with 4-HPR. Otolaryngol Head Neck Surg. 2005 Nov;133(5):695-701. doi: 10.1016/j.otohns.2005.07.019.
66 PPARgamma-mediated antineoplastic effect of NSAID sulindac on human oral squamous carcinoma cells. Int J Cancer. 2002 Apr 20;98(6):817-23.
67 Indomethacin and juglone inhibit inflammatory molecules to induce apoptosis in colon cancer cells. J Biochem Mol Toxicol. 2020 Feb;34(2):e22433. doi: 10.1002/jbt.22433. Epub 2020 Jan 9.
68 Telmisartan ameliorates lipopolysaccharide-induced innate immune response through peroxisome proliferator-activated receptor- activation in human monocytes. J Hypertens. 2012 Jan;30(1):87-96. doi: 10.1097/HJH.0b013e32834dde5f.
69 Cholesteryl ester-transfer protein inhibitors stimulate aldosterone biosynthesis in adipocytes through Nox-dependent processes. J Pharmacol Exp Ther. 2015 Apr;353(1):27-34.
70 In Vitro and In Vivo Characterizations of Chiglitazar, a Newly Identified PPAR Pan-Agonist. PPAR Res. 2012;2012:546548. doi: 10.1155/2012/546548. Epub 2012 Oct 22.
71 AZ 242, a novel PPARalpha/gamma agonist with beneficial effects on insulin resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats. J Lipid Res. 2002 Nov;43(11):1855-63. doi: 10.1194/jlr.m200127-jlr200.
72 Classification of heavy-metal toxicity by human DNA microarray analysis. Environ Sci Technol. 2007 May 15;41(10):3769-74.
73 Upregulation of SIRT1-AMPK by thymoquinone in hepatic stellate cells ameliorates liver injury. Toxicol Lett. 2016 Nov 16;262:80-91. doi: 10.1016/j.toxlet.2016.09.014. Epub 2016 Sep 26.
74 Gamma (gamma) tocopherol upregulates peroxisome proliferator activated receptor (PPAR) gamma (gamma) expression in SW 480 human colon cancer cell lines. BMC Cancer. 2003 Oct 1;3:25. doi: 10.1186/1471-2407-3-25.
75 PPAR gamma ligands, troglitazone and pioglitazone, up-regulate expression of HMG-CoA synthase and HMG-CoA reductase gene in THP-1 macrophages. FEBS Lett. 2002 Jun 5;520(1-3):177-81.
76 Comparative study of the effects of ziram and disulfiram on human monocyte-derived macrophage functions and polarization: involvement of zinc. Cell Biol Toxicol. 2021 Jun;37(3):379-400. doi: 10.1007/s10565-020-09540-6. Epub 2020 Jul 25.
77 Stable reporter cell lines for peroxisome proliferator-activated receptor (PPAR)-mediated modulation of gene expression. Anal Biochem. 2011 Jul 1;414(1):77-83. doi: 10.1016/j.ab.2011.02.032. Epub 2011 Feb 24.
78 PPAR mediates the anti-pulmonary fibrosis effect of icaritin. Toxicol Lett. 2021 Oct 10;350:81-90. doi: 10.1016/j.toxlet.2021.06.014. Epub 2021 Jun 18.
79 Impact of environmental chemicals on key transcription regulators and correlation to toxicity end points within EPA's ToxCast program. Chem Res Toxicol. 2010 Mar 15;23(3):578-90. doi: 10.1021/tx900325g.
80 Correlation between activation of PPAR and resistin downregulation in a mouse adipocyte cell line by a series of thiazolidinediones. Toxicol In Vitro. 2013 Aug;27(5):1425-32. doi: 10.1016/j.tiv.2013.03.011. Epub 2013 Apr 3.
81 Transcriptional signature of human macrophages exposed to the environmental contaminant benzo(a)pyrene. Toxicol Sci. 2010 Apr;114(2):247-59.
82 The BET bromodomain inhibitor JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models. Oncogene. 2016 Feb 18;35(7):833-45.
83 Inhibition of G-protein-coupled Receptor Kinase 2 Prevents the Dysfunctional Cardiac Substrate Metabolism in Fatty Acid Synthase Transgenic Mice. J Biol Chem. 2016 Feb 5;291(6):2583-600. doi: 10.1074/jbc.M115.702688. Epub 2015 Dec 15.