m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT02019
 [1]
DNA methylation DNMT1 FTO Direct Inhibition m6A modification PPARA PPARA FTO Demethylation : m6A sites
m6A Modification:
m6A Regulator Fat mass and obesity-associated protein (FTO) ERASER
 Regulator Info 
m6A Target Peroxisome proliferator-activated receptor alpha (PPARalpha/PPARA)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type DNA methylation (DNAMeth)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 1 (DNMT1) WRITER View Details
Regulated Target FTO alpha-ketoglutarate dependent dioxygenase (FTO) View Details
Crosstalk Relationship DNA methylation  →  m6A Inhibition
Crosstalk Mechanism DNA methylation directly impacts m6A modification through modulating the expression level of m6A regulator
Crosstalk Summary Inhibition of DNA methyltransferases (DNMT1, DNMT3A, and DNMT3B) by 5-azacytidine (5-aza) reversed alcohol-induced kidney injury and decreased the mRNA and protein levels of FTO. Importantly, we found that FTO, the m6A demethylase, epigenetically modified Peroxisome proliferator-activated receptor alpha (PPARalpha/PPARA) in a YTH domain family 2 (YTHDF2)-dependent manner, which resulted in inflammation in alcoholic kidney injury models. In conclusion, our findings indicate that alcohol increases the methylation of PPAR-alpha m6A by FTO-mediated YTHDF2 epigenetic modification, which ultimately leads to the activation of NLRP3 inflammasomes and NF-kappaB-driven renal inflammation in the kidney.
Responsed Disease Renal ischemia-reperfusion injury ICD-11: NB92.0Y
 Disease Info 
Responsed Drug 5-azacytidine
 Drug Info 
Pathway Response RNA degradation hsa03018
Cell Process mRNA stability
In-vitro Model
 HK2 Normal Acipenser baerii CVCL_YE28
In-vivo Model Male C57BL/6 mice (aged 6-8 weeks) were acclimated with the Lieber-DeCarli liquid diet control ad libitum for 1 week. Afterward, mice received either Lieber-DeCarli diet ethanol (6% vol/vol) or Lieber-DeCarli diet control (isocaloric maltose dextrin) for 4 and 8 weeks.
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
DNA (cytosine-5)-methyltransferase 1 (DNMT1) 27 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name SGI110 Phase 3 [2]
MOA Modulator
External Link
CID: 137295284
TTD: D0Q5KZ
 Compound Name Guadecitabine Phase 3 [3]
Synonyms
UNII-2KT4YN1DP7; 929901-49-5; 2KT4YN1DP7; SGI-110 free acid; Guadecitabine [USAN:INN]; GuadecitabineSGI-110; Guadecitabine (USAN/INN); CHEMBL3544916; Guanosine, 2'-deoxy-5-azacytidylyl-(3'-5')-2'-deoxy-; ZINC43203165; AKOS027321496; AKOS030238181; DB11918; CS-3089; HY-13542; D10877; 2'-deoxy-5-azacytidylyl-(3'-5')-2'-deoxyguanosine
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 135564655
TTD: D0VZ4N
DrugBank: DB11918
 Compound Name CC-486 Phase 3 [4]
Synonyms
AG-14361; AG14361; 328543-09-5; UNII-48N0U0K50I; AG 14361; CHEMBL65892; 48N0U0K50I; Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-; AG-014361; 1-(4-((dimethylamino)methyl)phenyl)-8,9-dihydro-2,7,9a-triazabenzo[cd]azulen-6(7H)-one; Imidazo(4,5,1-jk)(1,4)benzodiazepin-7(4H)-one, 2-(4-((dimethylamino)methyl)phenyl)-5,6-dihydro-; 2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one; SMR000486393; MLS006011157; MLS001065917; Nucleoside analogue
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 9840076
TTD: D09NTC
 Compound Name S-110 Phase 3 [5]
Synonyms
DNA demethylating agent (myelodysplastic syndrome), Supergen
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0A2BO
 Compound Name Palifosfamide Phase 2 [6]
Synonyms
ZIO-201
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 100427
TTD: D04FDN
DrugBank: DB05668
 Compound Name RX-3117 Phase 2 [7]
Synonyms
Antimetabolite (cancer), Rexahn; Antimetabolite (cancer), Rexahn/ Teva
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 11242315
TTD: D0L7WS
 Compound Name Antroquinonol Phase 2 [8]
Synonyms
Hocena; Fungal extract (cancer), Golden Biotechnology
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 24875259
TTD: D0T3AW
DrugBank: DB12326
 Compound Name GSK4172239 Phase 1 [9]
MOA Inhibitor
External Link
TTD: D5QR2M
 Compound Name PMID27376512-Compound-miR-155-5p Patented [10]
MOA Inhibitor
Activity Ki = 27.88 nM
External Link
TTD: D01CGQ
 Compound Name PMID27376512-Compound-Table1Example11 Patented [10]
MOA Inhibitor
Activity IC50 = 39440 nM
External Link
CID: 75201485
TTD: D04JIH
 Compound Name PMID27376512-Compound-Table1Example16 Patented [10]
MOA Inhibitor
Activity IC50 = 22520 nM
External Link
CID: 75201537
TTD: D05DSL
 Compound Name PMID27376512-Compound-Table1Example5 Patented [10]
MOA Inhibitor
Activity IC50(DNMT1) = 3530 nM
External Link
CID: 73774653
TTD: D09FMS
 Compound Name PMID27376512-Compound-asCEBP-2HPE Patented [10]
MOA Inhibitor
Activity Ki = 135.2 nM
External Link
TTD: D0E7OA
 Compound Name PMID27376512-Compound-asCEBP-1 Patented [10]
MOA Inhibitor
Activity Ki = 2003 nM
External Link
TTD: D0G6ON
 Compound Name PMID27376512-Compound-Table1Example4 Patented [10]
MOA Inhibitor
Activity IC50 = 13810 nM
External Link
CID: 75201432
TTD: D0K4YF
 Compound Name PMID27376512-Compound-asCEBP-2 Patented [10]
MOA Inhibitor
Activity Ki = 434.1 nM
External Link
TTD: D0KE4E
 Compound Name PMID27376512-Compound-asCEBP-1HPE Patented [10]
MOA Inhibitor
Activity Ki = 917.5 nM
External Link
TTD: D0LK4R
 Compound Name PMID27376512-Compound-Table1Example8 Patented [10]
MOA Inhibitor
Activity IC50 = 6850 nM
External Link
CID: 75201482
TTD: D0RT6C
 Compound Name PMID27376512-Compound-MTC-433 Patented [10]
MOA Inhibitor
Activity IC50 = 4.22 nM
External Link
TTD: D0U5CK
 Compound Name PMID27376512-Compound-Table1Example30 Patented [10]
MOA Inhibitor
External Link
CID: 75201638
TTD: D0YK6K
 Compound Name PMID27376512-Compound-MTC-424 Patented [10]
MOA Inhibitor
Activity IC50 = 1940 nM
External Link
TTD: D02WRM
 Compound Name PMID27376512-Compound-MTC-427 Patented [10]
MOA Inhibitor
Activity IC50 = 295 nM
External Link
TTD: D0HA0J
 Compound Name PMID27376512-Compound-MTC-422 Patented [10]
MOA Inhibitor
Activity IC50 = 1430 nM
External Link
TTD: D0QY0N
 Compound Name PMID27376512-Compound-MTC-423 Patented [10]
MOA Inhibitor
Activity IC50 = 363 nM
External Link
TTD: D0W9VZ
 Compound Name PMX-700 Investigative [11]
Synonyms
SJ-005019; SJ-005059; DC-010-116; Temozolomide analogs (cancer), Pharminox
    Click to Show/Hide
MOA Modulator
External Link
TTD: D03DTQ
 Compound Name XB-05 Investigative [11]
MOA Inhibitor
External Link
TTD: D0JV8Q
 Compound Name CP-4200 Investigative [11]
Synonyms
Lipidated azacitidine (cancer, Lipid Vector), Clavis Pharma; 5-azacytidine-5'-elaidate
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0OT1S
Peroxisome proliferator-activated receptor alpha (PPARalpha/PPARA) 76 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Bezafibrate Approved [12]
Synonyms
Azufibrat; Befibrat; Befizal; BezaLande; BezaPuren; Bezabeta; Bezacur; Bezafibrat; Bezafibrato; Bezafibratum; Bezafisal;Bezalip; Bezamerck; Bezatol; Cedur; Difaterol; Durabezur; Eulitop; Lipox; Reducterol; Sklerofibrat; Solibay; Azupharma Brand of Bezafibrate; Bayer Brand of Bezafibrate; Berlin Chemie Brand of Bezafibrate; Betapharm Brand of Bezafibrate; Beza Lande; Beza Puren; Bezafibrat PB; Bezafibrate Azupharma Brand; Bezafibrate Bayer Brand; Bezafibrate Betapharm Brand; Bezafibrate Cryopharma Brand; Bezafibrate Elfar Brand; Bezafibrate Hennig Brand; Bezafibrate Hexal Brand; Bezafibrate Isis Brand; Bezafibrate Lakeside Brand; Bezafibrate Merckle Brand; Bezafibrate Roche Brand; Bezafibrate Synthelabo Brand; Bezafibrate TAD Brand; Bezafibrate Teva Brand; Bezafibrato [Spanish]; Bezalip Retard; Bezatol SR; Boehringer Mannheim Brand of Bezafibrate; Cryopharma Brand of Bezafibrate; Elfar Brand of Bezafibrate;Hennig Brand of Bezafibrate; Hexal Brand of Bezafibrate; Isis Brand of Bezafibrate; Lakeside Brand of Bezafibrate; Merckle Brand of Bezafibrate; Regadrin B; Roche Brand of Bezafibrate; Synthelabo Brand of Bezafibrate; TAD Brand of Bezafibrate; Teva Brand of Bezafibrate; BM 15075; LO 44; BF-759; BM 15.075; BM-15075; BM15.075; Berlin-Chemie Brand of Bezafibrate; Beza-Lande; Beza-Puren; Bezafibrate Berlin-Chemie Brand; Bezafibrato [INN-Spanish]; Bezafibratum [INN-Latin]; Bezalip (TN); Bezatol SR (TN); PB, Bezafibrat; BM-15.075; Bezafibrate (JP15/USAN/INN); Bezafibrate [USAN:BAN:INN:JAN]; A-[4-(4-chlorobenzoylaminoethyl)phenoxy]isobutyric acid; 2-(4-{2-[(4-chlorobenzoyl)amino]ethyl}phenoxy)-2-methylpropanoic acid; 2-(p-(2-(p-Chlorobenzamido)ethyl)phenoxy)-2-methylpropionic acid; 2-[4-(2-[4-Chlorobenzamido]ethyl)-phenoxy]-2-methylpropanoic acid; 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropanoic acid; 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]isobutyric Acid; 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methylpropanoic acid
    Click to Show/Hide
MOA Agonist
Activity EC50 = 7100 nM
External Link
CID: 39042
TTD: D00WCX
DrugBank: DB01393
 Compound Name Pemafibrate Approved [13]
Synonyms
K-877
    Click to Show/Hide
MOA Agonist
Activity EC50 = 1 nM
External Link
CID: 11526038
TTD: D04QIE
DrugBank: DB15212
 Compound Name Fenofibrate Approved [14]
Synonyms
Ankebin; Antara; Controlip; Durafenat; Elasterate; Elasterin; FNF; Fenobeta; Fenobrate; Fenofanton; Fenofibrato; Fenofibratum; Fenogal; Fenoglide; Fenomax; Fenotard; Finofibrate; Fulcro; Lipanthyl; Lipantil; Liparison; Lipidex; Lipidil; Lipifen; Lipirex; Lipoclar; Lipofen; Lipofene; Liposit; Lipsin; Lofibra; Luxacor; Nolipax; Pharmavit; Phenofibrate; Procetofen; Procetofene; Proctofene; Protolipan; Secalip; Sedufen; Supralip; Tricor; Triglide; AbZ Brand of Procetofen; Abbott Brand of Procetofen; Aliud Brand of Procetofen; Antara Micronized Procetofen; Anto Brand of Procetofen; Apo Feno Micro; Apo Fenofibrate; Apotex Brand of Procetofen; Azupharma Brand of Procetofen; Betapharm Brand of Procetofen; Bouchara Brand of Procetofen; Ct Arzneimittel Brand of Procetofen; Fenofibrat AL; Fenofibrat AZU; Fenofibrat AbZ; Fenofibrat FPh; Fenofibrat Heumann; Fenofibrat Hexal; Fenofibrat Stada; Fenofibrat ratiopharm; Fenofibrat von ct; Fenofibrate Debat; Fenofibrate MSD; Fournier Brand of Procetofen; GNR Pharma Brand of Procetofen; Gate Brand of Procetofen; Gen Fenofibrate; Genpharm Brand of Procetofen; Heumann Brand of Procetofen; Hexal Brand of Procetofen; Knoll Brand of Procetofen; Lichtenstein Brand of Procetofen; Lipidil Micro; Lipidil Supra; Lipidil Ter; MTW Brand of Procetofen; MTW Fenofibrat; Merck dura Brand of Procetofen; Novartis Brand of Procetofen; Novo Fenofibrate; Novopharm Brand of Procetofen; Nu Fenofibrate; Nu Pharm Brand of Procetofen; PMS Fenofibrate Micro;Pharmascience Brand of Procetofen; Procetofen Reliant Brand; Q Pharm Brand of Procetofen; Ratiopharm Brand of Procetofen; Reliant Brand of Procetofen; Schering Plough Brand of Procetofen; Stadapharm Brand of Procetofen; United Drug Brand of Procetofen; F 6020; LF 178; LF178; AZU, Fenofibrat; Antara (TN); Antara (micronized); Apo-Fenofibrate; CIP-Fenofibrate; Ct-Arzneimittel Brand of Procetofen; Debat, Fenofibrate; FENOFIBRATE (MICRONIZED); Fenofibrat-ratiopharm; Fenofibrate IDD-P; Fenofibrate [INN:BAN]; Fenofibrato [INN-Spanish]; Fenofibratum [INN-Latin]; Fenogal (TN); GNR-Pharma Brand of Procetofen; GRS-027; Gen-Fenofibrate; Heumann, Fenofibrat; Hexal, Fenofibrat; LCP-Feno; LCP-FenoChol; LF-178; Lipanthyl (TN); Lipantil (TN); Lipidil (TN); Lipidil-Ter; Lipofen (TN); Lofibra (TN); MTW-Fenofibrat; Micronized Procetofen, Antara; Novo-Fenofibrate; Nu-Fenofibrate; Nu-Pharm Brand of Procetofen; PMS-Fenofibrate Micro; Procetofen, Antara Micronized; Q-Pharm Brand of Procetofen; Schering-Plough Brand of Procetofen; Stada, Fenofibrat; TRICOR (MICRONIZED); Tricor (TN); Triglide (TN); Trilipix (TN); Apo-Feno-Micro; Fenocor-67 (TN); Fenofibrate (JAN/INN); Isopropyl 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate; Isopropyl 2-(4-(4-chlorobenzoyl)phenoxy)-2-methylpropionate; Isopropyl 2-(p-(p-chlorobenzoyl)phenoxy)-2-methylpropionate
    Click to Show/Hide
MOA Agonist
Activity IC50 = 1000 nM
External Link
CID: 3339
TTD: D07XGR
DrugBank: DB01039
 Compound Name Ciprofibrate Approved [14]
Synonyms
Ciprofibrato; Ciprofibratum; Ciprol; Hiperlipen; Hyperlipen; Lipanor; Modalim; Oroxadin; Sanofi Synthelabo brand of ciprofibrate; Sanofi Winthrop brand of ciprofibrate; C 0330; WIN 35833; Ciprofibrato [INN-Spanish]; Ciprofibratum [INN-Latin]; Win 35,833; Win-35833; Ciprofibrate (USAN/INN); Ciprofibrate [USAN:BAN:INN]; 2-(4-(2,2-Dichlorocyclopropyl)phenoxy)2-methylpropanoic acid; 2-(p-(2,2-Dichlorocyclopropyl)phenoxy)-2-methylpropionic acid; 2-[4-(2,2-Dichlorocyclopropyl)phenoxy]-2-methylpropanoic acid; 2-[p-(2,2-Dichlorocyclopropyl)phenoxy]-2-methylpropanoic acid; 2-{4-[2,2-dichlorocyclopropyl]phenoxy}-2-methylpropanoic acid; 2-{[4-(2,2-dichlorocyclopropyl)phenyl]oxy}-2-methylpropanoic acid
    Click to Show/Hide
MOA Agonist
Activity EC50 = 900 nM
External Link
CID: 2763
TTD: D0EJ6O
DrugBank: DB09064
 Compound Name Lobeglitazone Approved [15]
Synonyms
Lobeglitazone sulfate; CKD-501; Dual PPARalpha/delta (type 2 diabetes), Chong Kun Dang
    Click to Show/Hide
MOA Agonist
External Link
CID: 9826451
TTD: D04BCB
DrugBank: DB09198
 Compound Name Ragaglitazar Phase 3 [16]
Synonyms
DRF-2725; (2S)-2-ETHOXY-3-{4-[2-(10H-PHENOXAZIN-10-YL)ETHOXY]PHENYL}PROPANOIC ACID; CHEMBL24038; (2S)-2-ethoxy-3-[4-(2-phenoxazin-10-ylethoxy)phenyl]propanoic acid; DRF; 1nyx; DRF2725; AC1L9KVW; 2-Ethoxy-3-[4-(2-phenoxazin-10-yl-ethoxy)-phenyl]-propionic acid; GTPL2664; SCHEMBL4822459; WMUIIGVAWPWQAW-DEOSSOPVSA-N; NN-622; BDBM50109551; DB07675; NNC-61-0029; (-)-DRF-2725; (S)-2-Ethoxy-3-[4-(2-phenoxazin-10-yl-ethoxy)-phenyl]-propionic acid; (2S)-2-ethoxy-3-{4-[2-(phenoxazin-10-yl)ethoxy]phenyl}propanoic acid
    Click to Show/Hide
MOA Modulator
Activity Ki = 980 nM
External Link
CID: 447458
TTD: D02NHD
DrugBank: DB07675
 Compound Name CS-038 Phase 3 [17]
Synonyms
Chiglitazar; CS-00098; PPAR alpha/gamma agonist (diabetes), Chipscreen Biosciences
    Click to Show/Hide
MOA Modulator
External Link
CID: 71402018
TTD: D0F5JH
 Compound Name TESAGLITAZAR Phase 3 [18]
Synonyms
251565-85-2; Galida; (S)-2-Ethoxy-3-(4-(4-((methylsulfonyl)oxy)phenethoxy)phenyl)propanoic acid; AZ 242; AZ-242; AR-H039242XX; (S)-2-Ethoxy-3-{4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl}propionic acid; UNII-6734037O3L; (S)-2-Ethoxy-3-{4-[2-(4-methanesulfonyloxy-phenyl)-ethoxy]-phenyl}-propionic acid; (2S)-2-ethoxy-3-[4-[2-(4-methylsulfonyloxyphenyl)ethoxy]phenyl]propanoic acid; BR-44608; 6734037O3L; (S)-2-Ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic acid
    Click to Show/Hide
MOA Modulator
Activity EC50 = 37 nM
External Link
CID: 208901
TTD: D0H1NL
DrugBank: DB07399
 Compound Name GFT-505 Phase 3 [19]
Synonyms
GFT-1007; PPAR activator (dyslipidemia/type 2 diabetes), Genfit
    Click to Show/Hide
MOA Modulator
Activity EC50 = 10 nM
External Link
CID: 9864881
TTD: D0LW1Y
DrugBank: DB05187
 Compound Name MURAGLITAZAR Phase 3 [20]
Synonyms
331741-94-7; Pargluva; BMS-298585; UNII-W1MKM70WQI; BMS 298585; W1MKM70WQI; CHEMBL186179; N-[(4-Methoxyphenoxy)carbonyl]-N-[[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine; N-((4-methoxyphenoxy)carbonyl)-N-((4-(2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy)phenyl)methyl)glycine; BMS298585; Muraglitazar [USAN:INN]; CCRIS 9258; AC1L4FVP; Muraglitazar (USAN/INN); DSSTox_CID_31508; DSSTox_RID_97393; DSSTox_GSID_57719; SCHEMBL676469; DTXSID9057719; CTK8E8901; MolPort-006-395-259; IRLWJILLXJGJTD-UHFFFAOYSA-N
    Click to Show/Hide
MOA Modulator
Activity EC50 = 40 nM
External Link
CID: 206044
TTD: D0M3UT
DrugBank: DB06510
 Compound Name ZYH-1 Phase 3 [21]
Synonyms
Metabolism disorder treatment, Zydus-Cadila; PPAR alpha/gamma modulator (dyslipdemia), Zydus-Cadila
    Click to Show/Hide
MOA Modulator
External Link
TTD: D0T7MN
 Compound Name Imiglitazar Phase 3 [22]
Synonyms
TAK-559
    Click to Show/Hide
MOA Modulator
Activity EC50 = 5 nM
External Link
CID: 9890879
TTD: D0VU5M
DrugBank: DB12511
 Compound Name LY-518674 Phase 2 [23]
Synonyms
LY-674; 2-Methyl-2-[4-[3-[1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl]propyl]phenoxy]propionic acid
    Click to Show/Hide
MOA Agonist
Activity EC50 = 42 nM
External Link
CID: 135449333
TTD: D0I5IM
DrugBank: DB12988
 Compound Name GFT14 Phase 2 [24]
MOA Agonist
External Link
TTD: D0RJ0V
 Compound Name ZYH7 Phase 2 [25]
MOA Agonist
External Link
TTD: DE6GF4
 Compound Name Naveglitazar Phase 2 [26]
Synonyms
LY 519818; LY-818; PPAR alpha/gamma co-agonists, Lilly/Ligand
    Click to Show/Hide
MOA Modulator
Activity EC50 = 2800 nM
External Link
CID: 9888484
TTD: D04BPS
DrugBank: DB12662
 Compound Name ONO-5129 Phase 2 [27]
Synonyms
Dual PPAR alpha/gamma agonist (metabolic disorder), Ono
    Click to Show/Hide
MOA Modulator
External Link
TTD: D0PP8G
 Compound Name CDT-fenofibrate Phase 1 [28]
MOA Agonist
External Link
TTD: D00HYD
 Compound Name AVE0897 Phase 1 [29]
MOA Agonist
External Link
TTD: D01UJK
 Compound Name TPST-1120 Phase 1 [30]
MOA Antagonist
External Link
TTD: DF8M1T
 Compound Name Oxeglitazar Phase 1 [31]
Synonyms
EMD-336340; EML-16156; EML-4156; LM-4156
    Click to Show/Hide
MOA Modulator
External Link
CID: 6445229
TTD: D03RJZ
 Compound Name GW-409544 Phase 1 [32]
Synonyms
GW-409544X; GW-544; GW-6471; Lipid regulators, Ligand/Glaxo
    Click to Show/Hide
MOA Modulator
Activity Ki = 2 nM
External Link
CID: 446642
TTD: D0AX9S
 Compound Name PMID25416646-Compound-Figure5-H Patented [33]
MOA Agonist
External Link
TTD: D05AUY
 Compound Name Flavonoid derivative 8 Patented [33]
Synonyms
PMID25416646-Compound-Figure5-B
    Click to Show/Hide
MOA Agonist
External Link
TTD: D0HW6Y
 Compound Name PMID25416646-Compound-Figure5-A Patented [33]
MOA Agonist
External Link
TTD: D0O5IN
 Compound Name Aleglitazar Discontinued in Phase 3 [34]
Synonyms
RO7; Aleglitazar (USAN); 2-methoxy-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]benzothiophen-7-yl]propanoic Acid
    Click to Show/Hide
MOA Agonist
Activity EC50 = 50 nM
External Link
CID: 10274777
TTD: D0B9EN
DrugBank: DB08915
 Compound Name NS-220 Discontinued in Phase 2 [35]
Synonyms
R-1593; Cis-2-Methyl-5-[4-[5-methyl-2-(4-methylphenyl)oxazol-4-yl]butyl]-1,3-dioxane-2-carboxylic acid
    Click to Show/Hide
MOA Agonist
Activity EC50 = 10 nM
External Link
CID: 9947731
TTD: D08LZI
 Compound Name KRP-101 Discontinued in Phase 2 [36]
Synonyms
PPAR alpha agonist (hyperlipidemia), Kyorin
    Click to Show/Hide
MOA Agonist
Activity EC50 = 0.615 nM
External Link
CID: 9825046
TTD: D0B8JQ
 Compound Name BM-17.0744 Discontinued in Phase 2 [37]
Synonyms
K-111; 12-(4-Chlorophenyl)-2,2-dichlorododecanoic acid
    Click to Show/Hide
MOA Activator
External Link
CID: 9929731
TTD: D0Q8UU
 Compound Name AVE-8134 Discontinued in Phase 2 [38]
Synonyms
PPAR alpha agonist, Genfit
    Click to Show/Hide
MOA Agonist
External Link
CID: 11625114
TTD: D0R5QQ
 Compound Name KRP-297 Discontinued in Phase 2 [39]
Synonyms
MK 767; MK-767; KRP297; KRP 297; 213252-19-8; L410198; L 410198; 5-((2,4-Dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)benzamide; Benzamide, 5-((2,4-dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)-; 5-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]-2-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]benzamide; NFFXEUUOMTXWCX-UHFFFAOYSA-N; SCHEMBL3922; AC1L45TL; MLS006010319; GTPL2677; CTK4E6495; MolPort-018-657-358; AKOS005067111; NCGC00263123-01; SMR004701384
    Click to Show/Hide
MOA Modulator
External Link
CID: 151183
TTD: D02RAU
 Compound Name Reglixane Discontinued in Phase 2 [27]
MOA Modulator
External Link
TTD: D02ZKL
 Compound Name AVE-0847 Discontinued in Phase 2 [40]
Synonyms
PPAR alpha/gamma agonists (diabetes/dyslipidemia), Genfit; PPAR alpha/gamma agonists (diabetes/dyslipidemia), aventis; PPAR alpha/gamma agonists (diabetes/dyslipidemia), sanofi-aventis
    Click to Show/Hide
MOA Modulator
External Link
TTD: D0W2IU
 Compound Name Sodelglitazar Discontinued in Phase 2 [41]
Synonyms
447406-78-2; UNII-6G973E04VI; 6G973E04VI; GW677954; Sodelglitazar [USAN:INN]; 2-[4-[[[2-[2-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-1,3-thiazol-5-yl]methyl]sulfanyl]-2-methylphenoxy]-2-methylpropanoic acid; 2-(4-(((2-(2-Fluoro-4-(trifluoromethyl)phenyl)-4-methyl-1,3-thiazol-5-yl)methyl)sulfanyl)-2-methylphenoxy)-2-methylpropanoic acid; Sodelglitazar (USAN); SCHEMBL4822839; CHEMBL2104984; DTXSID90196289; ZUGQWAYOWCBWGM-UHFFFAOYSA-N; ZINC1553281; AN-28238; ACM447406782; FT-0743554; D06647; 406S782; Propanoic ac
    Click to Show/Hide
MOA Agonist
External Link
CID: 9805950
TTD: D01JGG
 Compound Name Indeglitazar Discontinued in Phase 2 [42]
Synonyms
PLX-204
    Click to Show/Hide
MOA Agonist
External Link
CID: 11395145
TTD: D09OHP
DrugBank: DB07724
 Compound Name GSK-677954 Discontinued in Phase 2 [43]
Synonyms
SCHEMBL2065429
    Click to Show/Hide
MOA Agonist
External Link
CID: 56603715
TTD: D0S6KX
 Compound Name AR-H049020 Discontinued in Phase 1 [44]
MOA Agonist
External Link
TTD: D04FTB
 Compound Name LG-101280 Discontinued in Phase 1 [45]
Synonyms
LSN-862; LY-WWW; LY-YYY; PPAR modulators, Ligand/Lilly
    Click to Show/Hide
MOA Modulator
External Link
TTD: D09SLU
 Compound Name DRF 10945 Discontinued in Phase 1 [46]
MOA Agonist
External Link
TTD: D0W3YW
 Compound Name MP-136 Discontinued in Phase 1 [47]
MOA Agonist
External Link
TTD: D0Z3XO
 Compound Name E-3030 Discontinued in Phase 1 [48]
Synonyms
Dual PPAR alpha/gamma agonists, Eisai
    Click to Show/Hide
MOA Modulator
External Link
CID: 11949481
TTD: D06PHO
 Compound Name LY-929 Discontinued in Phase 1 [49]
Synonyms
LY-510929; Dual PPAR-alpha/PPAR-gamma agonists
    Click to Show/Hide
MOA Agonist
Activity EC50 = 8.913 nM
External Link
CID: 9890585
TTD: D0B0EB
 Compound Name MC-3001 Preclinical [50]
Synonyms
MC-3004; PPAR-alpha agonists, MaxoCore
    Click to Show/Hide
MOA Agonist
External Link
TTD: D04PBS
 Compound Name PIRINIXIC ACID Preclinical [51]
Synonyms
50892-23-4; WY-14643; [4-Chloro-6-(2,3-xylidino)-2-pyrimidinylthio]acetic acid; WY-14,643; WY14643; Wyeth 14,643; Wy 14643; Pirinixic acid [INN]; WY-14643 (Pirinixic Acid); (4-Chloro-6-(2,3-xylidino)-2-pyrimidinylthio)acetic acid; UNII-86C4MRT55A; C14H14ClN3O2S; CCRIS 133; Acidum pirinixicum [INN-Latin]; Acide pirinixique [INN-French]; Acido pirinixico [INN-Spanish]; NSC310038; NSC-310038; NSC 310038; BRN 0759945; ((4-Chloro-6-((2,3-dimethylphenyl)amino)-2-pyrimidinyl)thio)acetic acid; Acetic acid, ((4-chloro-6-(
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 130 nM
External Link
CID: 5694
TTD: D09XCX
 Compound Name Romazarit Preclinical [52]
Synonyms
ORE-5007; Metabolic modulator (obesity/hyperlipidemia), Ore Pharmaceuticals
    Click to Show/Hide
MOA Modulator
External Link
CID: 71321
TTD: D0U2FN
 Compound Name MC-3002 Preclinical [27]
Synonyms
PPAR dual agonists, MaxoCore
    Click to Show/Hide
MOA Modulator
External Link
TTD: D08WOE
 Compound Name CS-207 Terminated [53]
Synonyms
CS-307; PPAR alpha agonists (cardiovascular disease associated with dyslipidemia); PPAR alpha agonists (cardiovascular disease associated with dyslipidemia), Chipscreen Biosciences
    Click to Show/Hide
MOA Agonist
External Link
TTD: D03CUS
 Compound Name KRP-105 Terminated [54]
MOA Agonist
External Link
TTD: D0BB1X
 Compound Name BVT-142 Terminated [55]
Synonyms
BVT-13; BVT-142 analogs, Biovitrum; Dual PPAR alpha/gamma agonists (type II diabetes); Dual PPAR alpha/gamma agonists (type II diabetes), Biovitrum
    Click to Show/Hide
MOA Agonist
External Link
TTD: D0I0RF
 Compound Name Sipoglitazar Terminated [21]
Synonyms
TAK-654
    Click to Show/Hide
MOA Modulator
External Link
CID: 9825652
TTD: D0OW6Z
 Compound Name CS-204 Terminated [56]
Synonyms
CS-00088; PPAR alpha/gamma/delta agonist (type 2 diabetes), Chipscreen Bioscience
    Click to Show/Hide
MOA Agonist
External Link
TTD: D0V0TT
 Compound Name GW7647 Investigative [57]
Synonyms
GW-7647; GW 7647
    Click to Show/Hide
MOA Agonist
Activity Ki = 0.0541 nM
External Link
CID: 3392731
TTD: D00TFA
 Compound Name CP-775146 Investigative [58]
Synonyms
CP775146
    Click to Show/Hide
MOA Agonist
External Link
CID: 10410059
TTD: D01KPN
 Compound Name GSK-9578 Investigative [14]
Synonyms
KYQNYMXQHLMADB-UHFFFAOYSA-N; GW 9578; GW9578; 247923-29-1; GW-9578; UNII-H32ABL87X4; H32ABL87X4; CHEMBL278590; SCHEMBL68327; GTPL2673; BDBM28799; CTK8E7867; GSK9578; DTXSID10179493; MolPort-009-019-367; ZINC14115100; Propanoic acid, 2-((4-(2-((((2,4-difluorophenyl)amino)carbonyl)heptylamino)ethyl)phenyl)thio)-2-methyl-; RT-013144; J-015674; 289722-11-8; 2-{[4-(2-{[(2,4-difluorophenyl)carbamoyl](heptyl)amino}ethyl)phenyl]sulfanyl}-2-methylpropanoic acid; 2-[4-[2-[(2,4-difluorophenyl)carbamoyl-heptylamino]ethyl]phenyl]sulfanyl-2-methylpropanoic
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 6 nM
External Link
CID: 9870304
TTD: D05CLM
 Compound Name Fibrates Investigative [59]
Synonyms
clofibric acid; 882-09-7; 2-(4-Chlorophenoxy)-2-methylpropanoic acid; Chlorofibrinic acid; Clofibrinic acid; Chlorfibrinic acid; Clofibrin; 2-(4-CHLOROPHENOXY)-2-METHYLPROPIONIC ACID; Chlorophibrinic acid; PCIB; Clofibrate free acid; Clofibrinsaeure; Regulipid; Regadrin; PCPIB; 2-(p-Chlorophenoxy)-2-methylpropionic acid; 2-(4-Chlorophenoxy)isobutyric Acid; 4-CPIB; 2-(p-Chlorophenoxy)isobutyric acid; Propanoic acid, 2-(4-chlorophenoxy)-2-methyl-; alpha-(p-Chlorophenoxy)isobutyric acid; Acido clofibrico; Acide clofibrique; Acidum c
    Click to Show/Hide
MOA Agonist
Activity EC50 = 39600 nM
External Link
CID: 2797
TTD: D06RRD
 Compound Name BMS-687453 Investigative [60]
Synonyms
1000998-59-3; UNII-39TL5L7XDX; BMS 687453; 39TL5L7XDX; 2-{[(3-{[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}phenyl)methyl](methoxycarbonyl)amino}acetic acid; SCHEMBL2742714; CHEMBL1089501; BDBM28800; EX-A592; BCP14808; ZINC44460341; AKOS030526188; CS-5523; DA-48472; HY-10678; FT-0749275; J-690001; 2-[[3-[[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy]phenyl]methyl-methoxycarbonylamino]acetic acid; 7HA; N-(3-{[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}benzyl)-N-(methoxycarbonyl)glycine
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 9.6 nM
External Link
CID: 16725047
TTD: D08UWZ
 Compound Name pristanic acid Investigative [61]
Synonyms
UNII-6P06977L1A; 6P06977L1A; (2S,6R,10R)-2,6,10,14-tetramethylpentadecanoic acid; L,d,D-pristanic acid; GTPL2676; Pristanic acid, (2S,6R,10R)-; UNII-5FMQ2908AP component PAHGJZDQXIOYTH-KURKYZTESA-N; Pentadecanoic acid, 2,6,10,14-tetramethyl-, (2S,6R,10R)-
    Click to Show/Hide
MOA Agonist
External Link
CID: 123929
TTD: D0EN7T
 Compound Name eicosatetranoic acid Investigative [62]
Synonyms
ETYA; 5,8,11,14-eicosatetraynoic acid; 1191-85-1; icosa-5,8,11,14-tetraynoic acid; Octadehydroarachidonic acid; MLS000069514; SMR000058640; MLS-0002886.0001; Ro 31428; Ro 3-1428; Opera_ID_402; AC1Q5VYB; Spectrum5_001952; cid_1780; CBiol_001864; SCHEMBL68751; KBioSS_000169; BSPBio_001449; KBioGR_000169; GTPL2669; CHEMBL458328; BML2-F04; AC1L1C80; CTK0H5766; CHEBI:94483; KBio3_000338; KBio2_002737; KBio3_000337; KBio2_005305; KBio2_000169; BDBM31752; DTXSID20152318; MGLDCXPLYOWQRP-UHFFFAOYSA-N; HMS3402I11; Bio1_001128
    Click to Show/Hide
MOA Agonist
External Link
CID: 1780
TTD: D0G9IP
 Compound Name 8S-HETE Investigative [63]
Synonyms
8-hydroxyeicosatetraenoic acid
    Click to Show/Hide
MOA Agonist
External Link
CID: 5283154
TTD: D0K6TI
 Compound Name LL-6531 Investigative [47]
Synonyms
PPAR modulators (diabetes), Lupin
    Click to Show/Hide
MOA Modulator
External Link
TTD: D0K8HA
 Compound Name Deoxy-Bigchap Investigative [64]
Synonyms
Big CHAP, Deoxy; N,N-bis-(3-D-Gluconamidopropyl)deoxycholamide; AC1MTX5H; DTXSID70394140; AN-35629; FT-0629429; N,N -Bis(3-D -gluconamidopropyl)- deoxy-cholamide; N-[3-[4-(3,12-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanoyl-[3-(2,3,4,5,6-pentahydroxyhexanoylamino)propyl]amino]propyl]-2,3,4,5,6-pentahydroxyhexanamide
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 446320
TTD: D0S4GK
DrugBank: DB01890
 Compound Name (E)-4-(3,5-dimethoxystyryl)phenol Investigative [47]
Synonyms
Pterostilbene; 537-42-8; 4-(3,5-Dimethoxystyryl)phenol; 3',5'-Dimethoxy-4-stilbenol; trans-pterostilbene; 4-[(E)-2-(3,5-dimethoxyphenyl)ethenyl]phenol; pterostilben; 4-[(E)-2-(3,5-dimethoxyphenyl)vinyl]phenol; UNII-26R60S6A5I; 3,5-Dimethoxy-4'-hydroxy-trans-stilbene; 3,5-Dimethoxy-4'-hydroxystilbene; 18259-15-9; trans-3,5-dimethoxy-4'-hydroxystilbene; CHEMBL83527; CHEBI:8630; VLEUZFDZJKSGMX-ONEGZZNKSA-N; 4-((E)-2-(3,5-dimethoxyphenyl)ethenyl)phenol; 26R60S6A5I; Pterostilbene, Pterocarpus
    Click to Show/Hide
MOA Agonist
External Link
CID: 5281727
TTD: D00AII
 Compound Name AD-5061 Investigative [22]
Synonyms
AD-7057; AD7057; AD 7057; AD5061; AD 5061
    Click to Show/Hide
MOA Agonist
External Link
CID: 9953271
TTD: D00EOP
 Compound Name GW-2331 Investigative [65]
Synonyms
190844-95-2; PPAR ligand, Glaxo Wellcome
    Click to Show/Hide
MOA Modulator
Activity EC50 < 20 nM
External Link
CID: 657048
TTD: D01POG
 Compound Name TZD18 Investigative [66]
Synonyms
TZD 18; TZD-18
    Click to Show/Hide
MOA Agonist
External Link
CID: 9827261
TTD: D04JOG
 Compound Name (9Z,12E)-12-nitrooctadeca-9,12-dienoic acid Investigative [67]
Synonyms
12-Nitrolinoleic acid; 12-Nitro-9Z,12Z-octadecadienoic acid; CHEMBL554608; CHEBI:34150; AC1NQZV1; C13958; SCHEMBL2371323; BDBM50295045; LMFA01120002; 12-Nitro-9-cis,12-cis-octadecadienoic acid; (9Z,12Z)-12-Nitrooctadeca-9,12-dienoic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 9600 nM
External Link
CID: 5282316
TTD: D06GYO
 Compound Name reglitazar Investigative [68]
Synonyms
JTT-501
    Click to Show/Hide
MOA Agonist
External Link
CID: 154000
TTD: D08XGH
DrugBank: DB04971
 Compound Name DRF 2519 Investigative [69]
Synonyms
5-[[4-[2-(4-Oxo-2H-1,3-benzoxazin3(4H)-yl)ethoxy]phenyl]methyl2,4-thiazolidinedione; SCHEMBL6953746; GTPL2671; CHEMBL1491825; DTXSID5040754; NOCAS_40754; CTK8F9377; API0008459; NCGC00165785-01; NCGC00164420-01; SR-05000000444; SR-05000000444-2
    Click to Show/Hide
MOA Agonist
External Link
CID: 9908833
TTD: D0M8VN
 Compound Name (E)-12-Nitrooctadec-12-enoic Acid Investigative [67]
Synonyms
CHEMBL549351; BDBM50295043; (E)-12-Nitro-12-octadecenoic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1600 nM
External Link
CID: 44221100
TTD: D0M9LL
 Compound Name (E)-13-Nitrooctadec-12-enoic Acid Investigative [67]
Synonyms
CHEMBL540732
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1100 nM
External Link
CID: 44221101
TTD: D0P5QM
 Compound Name ZY H2 Investigative [70]
Synonyms
ZYH2
    Click to Show/Hide
MOA Modulator
External Link
TTD: D0Z4MH
 Compound Name LY-465608 Investigative [71]
Synonyms
LY465608; LY 465608
    Click to Show/Hide
MOA Agonist
Activity EC50 = 149.5 nM
External Link
CID: 9890319
TTD: D0Z7OX
 Compound Name DB-900 Investigative [72]
MOA Agonist
External Link
TTD: D01ARG
 Compound Name L-796449 Investigative [73]
Synonyms
UNII-O937X0Z5EM; CHEMBL278994; O937X0Z5EM; 194608-80-5; KAPDPGZDHUCILF-UHFFFAOYSA-N; GTPL2689; SCHEMBL4296303; BDBM50085040; Benzeneacetic acid, 3-chloro-4-((3-((3-phenyl-7-propyl-6-benzofuranyl)oxy)propyl)thio)-; L796449; L 796449; L-796,449; 3-chloro-4-(3-(3-phenyl-7-propylbenzofuran-6-yloxy)propylthio)-phenylacetic acid; {3-Chloro-4-[3-(3-phenyl-7-propyl-benzofuran-6-yloxy)-propylsulfanyl]-phenyl}-acetic acid; 2-[3-chloro-4-[3-[(3-phenyl-7-propyl-1-benzofuran-6-yl)oxy]propylsulfanyl]phenyl]acetic acid
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 4.1 nM
External Link
CID: 9891946
TTD: D09JII
 Compound Name L-165461 Investigative [73]
Synonyms
CHEMBL279053; SCHEMBL6753428; GTPL2690; BDBM50126016; AKOS027321335; L165461; L 165461; 3-Chloro-4-[3-(3-ethyl-7-propyl-1,2-benzisoxazole-6-yloxy)propylthio]benzeneacetic acid; 2-(3-chloro-4-(3-(3-ethyl-7-propylbenzo[d]isoxazol-6-yloxy)propylthio)phenyl)acetic acid; {3-Chloro-4-[3-(3-ethyl-7-propyl-benzo[d]isoxazol-6-yloxy)-propylsulfanyl]-phenyl}-acetic acid; 2-[3-chloro-4-[3-[(3-ethyl-7-propyl-1,2-benzoxazol-6-yl)oxy]propylsulfanyl]phenyl]acetic acid
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 247 nM
External Link
CID: 9889841
TTD: D0F0MP
 Compound Name N-oleoylethanolamide Investigative [74]
Synonyms
n-Oleoylethanolamine; oleoylethanolamide; N-(2-Hydroxyethyl)oleamide; 111-58-0; Oleylethanolamide; N-oleoyl ethanolamine; Oleamide MEA; Oleoyl monoethanolamide; Oleoyl Ethanolamide; N-(2-Hydroxyethyl)-9-octadecenamide; N-(Hydroxyethyl)oleamide; UNII-1HI5J9N8E6; (Z)-N-(2-hydroxyethyl)octadec-9-enamide; Oleic acid ethanolamide; N-(9Z-octadecenoyl)-ethanolamine; EINECS 203-884-8; OEA; MLS002153155; CHEMBL280065; 1HI5J9N8E6; (9Z)-N-(2-hydroxyethyl)octadec-9-enamide; Monoethanolamine oleic acid amide; CHEBI:71466; NOE
    Click to Show/Hide
MOA Agonist
Activity EC50 = 110 nM
External Link
CID: 5283454
TTD: D07MBC
References
Ref 1 DNA methylation of FTO promotes renal inflammation by enhancing m(6)A of PPAR-alpha in alcohol-induced kidney injury. Pharmacol Res. 2021 Jan;163:105286. doi: 10.1016/j.phrs.2020.105286. Epub 2020 Nov 4.
Ref 2 Immunomodulatory action of the DNA methyltransferase inhibitor SGI-110 in epithelial ovarian cancer cells and xenografts. Epigenetics. 2015;10(3):237-46.
Ref 3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 4 Efficacy and safety of extended dosing schedules of CC-486 (oral azacitidine) in patients with lower-risk myelodysplastic syndromes. Leukemia. 2016 Apr;30(4):889-96.
Ref 5 S110, a 5-Aza-2'-deoxycytidine-containing dinucleotide, is an effective DNA methylation inhibitor in vivo and can reduce tumor growth. Mol Cancer Ther. 2010 May;9(5):1443-50.
Ref 6 Anticancer activity of stabilized palifosfamide in vivo: schedule effects, oral bioavailability, and enhanced activity with docetaxel and doxorubicin. Anticancer Drugs. 2012 Feb;23(2):173-84.
Ref 7 Metabolism, mechanism of action and sensitivity profile of fluorocyclopentenylcytosine (RX-3117; TV-1360). Invest New Drugs. 2013 Dec;31(6):1444-57.
Ref 8 Antroquinonol D, isolated from Antrodia camphorata, with DNA demethylation and anticancer potential. J Agric Food Chem. 2014 Jun 18;62(24):5625-35.
Ref 9 Clinical pipeline report, company report or official report of GlaxoSmithKline
Ref 10 DNA methyltransferase inhibitors: an updated patent review (2012-2015). Expert Opin Ther Pat. 2016 Sep;26(9):1017-30. doi: 10.1080/13543776.2016.1209488. Epub 2016 Jul 18.
Ref 11 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2605).
Ref 12 Bezafibrate at clinically relevant doses decreases serum/liver triglycerides via down-regulation of sterol regulatory element-binding protein-1c in mice: a novel peroxisome proliferator-activated receptor alpha-independent mechanism. Mol Pharmacol. 2009 Apr;75(4):782-92. doi: 10.1124/mol.108.052928. Epub 2009 Jan 5.
Ref 13 Pemafibrate: First Global Approval. Drugs. 2017 Oct;77(16):1805-1810. doi: 10.1007/s40265-017-0818-x.
Ref 14 Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42. doi: 10.1074/jbc.275.22.16638.
Ref 15 Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-Gamma agonist, after a single oral administration in healthy female subjects. Clin Drug Investig. 2014 Jul;34(7):467-74. doi: 10.1007/s40261-014-0197-y.
Ref 16 Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes. J Clin Pharmacol. 2003 Nov;43(11):1244-56. doi: 10.1177/0091270003257230.
Ref 17 Determination of chiglitazar, a dual alpha/gamma peroxisome proliferator-activated receptor (PPAR) agonist, in human plasma by liquid chromatography-tandem mass spectrometry. Pharmazie. 2007 Nov;62(11):825-9.
Ref 18 Tesaglitazar, a dual PPAR-Alpha/Gamma agonist, hamster carcinogenicity, investigative animal and clinical studies. Toxicol Pathol. 2012;40(1):18-32. doi: 10.1177/0192623311429972. Epub 2011 Nov 30.
Ref 19 Dual peroxisome proliferator-activated receptor Alpha/Delta agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects. Diabetes Care. 2013 Oct;36(10):2923-30. doi: 10.2337/dc12-2012. Epub 2013 May 28.
Ref 20 Muraglitazar, a dual (alpha/gamma) PPAR activator: a randomized, double-blind, placebo-controlled, 24-week monotherapy trial in adult patients with type 2 diabetes. Clin Ther. 2005 Aug;27(8):1181-95. doi: 10.1016/j.clinthera.2005.08.005.
Ref 21 Pharmacokinetics, safety, and tolerability of saroglitazar (ZYH1), a predominantly PPARAlpha agonist with moderate PPARGamma agonist activity in healthy human subjects. Clin Drug Investig. 2013 Nov;33(11):809-16. doi: 10.1007/s40261-013-0128-3.
Ref 22 A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. Eur J Pharmacol. 2004 Jul 8;495(1):17-26. doi: 10.1016/j.ejphar.2004.05.020.
Ref 23 Potent and selective PPAR-alpha agonist LY518674 upregulates both ApoA-I production and catabolism in human subjects with the metabolic syndrome. Arterioscler Thromb Vasc Biol. 2009 Jan;29(1):140-6. doi: 10.1161/ATVBAHA.108.171223. Epub 2008 Nov 6.
Ref 24 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024296)
Ref 25 Clinical pipeline report, company report or official report of Zydus Cadila.
Ref 26 The disposition and metabolism of naveglitazar, a peroxisome proliferator-activated receptor alpha-gamma dual, gamma-dominant agonist in mice, rats, and monkeys. Drug Metab Dispos. 2007 Jan;35(1):51-61. doi: 10.1124/dmd.106.012328. Epub 2006 Sep 29.
Ref 27 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics. 2005 Aug;86(2):127-41. doi: 10.1016/j.ygeno.2005.04.008.
Ref 28 Mechanism of action of fibrates on lipid and lipoprotein metabolism. Circulation. 1998 Nov 10;98(19):2088-93. doi: 10.1161/01.cir.98.19.2088.
Ref 29 Pharma & Vaccines. Product Development Pipeline. April 29 2009.
Ref 30 Clinical pipeline report, company report or official report of Tempest Therapeutics.
Ref 31 Therapeutic potential of aleglitazar, a new dual PPAR-Alpha/Gamma agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16. doi: 10.2165/11539500-000000000-00000.
Ref 32 Design novel dual agonists for treating type-2 diabetes by targeting peroxisome proliferator-activated receptors with core hopping approach. PLoS One. 2012;7(6):e38546. doi: 10.1371/journal.pone.0038546. Epub 2012 Jun 7.
Ref 33 PPARGamma ligands and their therapeutic applications: a patent review (2008 - 2014). Expert Opin Ther Pat. 2015 Feb;25(2):175-91. doi: 10.1517/13543776.2014.985206. Epub 2014 Nov 21.
Ref 34 Clinical pipeline report, company report or official report of Roche (2009).
Ref 35 Modulation of PPAR receptor subtype selectivity of the ligands: aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6471-5. doi: 10.1016/j.bmcl.2008.10.062. Epub 2008 Oct 17.
Ref 36 Identification of a functional peroxisome proliferator-activated receptor (PPAR) response element (PPRE) in the human apolipoprotein A-IV gene. Biochem Pharmacol. 2009 Sep 1;78(5):523-30. doi: 10.1016/j.bcp.2009.05.007. Epub 2009 May 9.
Ref 37 Cardiac function and metabolism in Type 2 diabetic mice after treatment with BM 17.0744, a novel PPAR-alpha activator. Am J Physiol Heart Circ Physiol. 2002 Sep;283(3):H949-57. doi: 10.1152/ajpheart.00226.2001.
Ref 38 The peroxisome proliferator-activated receptor-alpha (PPAR-alpha) agonist, AVE8134, attenuates the progression of heart failure and increases survival in rats. Acta Pharmacol Sin. 2009 Jul;30(7):935-46. doi: 10.1038/aps.2009.58. Epub 2009 Jun 8.
Ref 39 [KRP-297, MCC-555]. Nihon Rinsho. 2001 Nov;59(11):2200-6.
Ref 40 DOI: 10.1038/scibx.2012.669
Ref 41 Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar. Protein Pept Lett. 2011 Oct;18(10):1021-7. doi: 10.2174/092986611796378701.
Ref 42 Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent. Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. doi: 10.1073/pnas.0811325106. Epub 2008 Dec 30.
Ref 43 Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58. doi: 10.1517/14728214.13.1.145.
Ref 44 CN patent application no. 100577175, Combination therapy comprising glucose reabsorption inhibitors and PPAR modulators.
Ref 45 A peroxisome proliferator-activated receptor alpha/gamma dual agonist with a unique in vitro profile and potent glucose and lipid effects in rodent models of type 2 diabetes and dyslipidemia. Mol Endocrinol. 2005 Jun;19(6):1593-605. doi: 10.1210/me.2005-0015. Epub 2005 Apr 14.
Ref 46 Peroxisome proliferator-activated receptors, metabolic syndrome and cardiovascular disease. Future Cardiol. 2010 September; 6(5): 657-691.
Ref 47 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 593).
Ref 48 Antidiabetic and hypolipidemic effects of a novel dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist, E3030, in db/db mice and beagle dogs. J Pharmacol Sci. 2008 Sep;108(1):40-8. doi: 10.1254/jphs.fp0072346. Epub 2008 Sep 6.
Ref 49 CN patent application no. 1882326, Ppar agonists for the treatment of hcv infection.
Ref 50 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021175)
Ref 51 O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3185-90. doi: 10.1016/s0960-894x(03)00702-9.
Ref 52 Fibrates as therapy for osteoarthritis and rheumatoid arthritis A systematic review. Ther Adv Musculoskelet Dis. 2013 February; 5(1): 33-44.
Ref 53 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026848)
Ref 54 Discovery of cyclic amine-substituted benzoic acids as PPARAlpha agonists. Bioorg Med Chem Lett. 2012 Jan 1;22(1):334-8. doi: 10.1016/j.bmcl.2011.11.002. Epub 2011 Nov 9.
Ref 55 A new class of peroxisome proliferator-activated receptor agonists with a novel binding epitope shows antidiabetic effects. J Biol Chem. 2004 Sep 24;279(39):41124-30. doi: 10.1074/jbc.M401552200. Epub 2004 Jul 15.
Ref 56 Peroxisome Proliferators-Activated Receptor (PPAR) Modulators and Metabolic Disorders. PPAR Res. 2008; 2008: 679137.
Ref 57 Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis. Bioorg Med Chem Lett. 2001 May 7;11(9):1225-7. doi: 10.1016/s0960-894x(01)00188-3.
Ref 58 Molecular characterization of novel and selective peroxisome proliferator-activated receptor alpha agonists with robust hypolipidemic activity in vivo. Mol Pharmacol. 2009 Feb;75(2):296-306. doi: 10.1124/mol.108.051656. Epub 2008 Oct 29.
Ref 59 Emerging antidyslipidemic drugs. Expert Opin Emerg Drugs. 2008 Jun;13(2):363-81. doi: 10.1517/14728214.13.2.363.
Ref 60 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. 2010 Apr 8;53(7):2854-64. doi: 10.1021/jm9016812.
Ref 61 Pristanic acid and phytanic acid: naturally occurring ligands for the nuclear receptor peroxisome proliferator-activated receptor alpha. J Lipid Res. 2000 Nov;41(11):1801-7.
Ref 62 PPAR alpha structure-function relationships derived from species-specific differences in responsiveness to hypolipidemic agents. Biol Chem. 1997 Jul;378(7):651-5. doi: 10.1515/bchm.1997.378.7.651.
Ref 63 Differential activation of peroxisome proliferator-activated receptors by eicosanoids. J Biol Chem. 1995 Oct 13;270(41):23975-83. doi: 10.1074/jbc.270.41.23975.
Ref 64 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 65 PPAR-alpha and -gamma but not -delta agonists inhibit airway inflammation in a murine model of asthma: in vitro evidence for an NF-kappaB-independent effect. Br J Pharmacol. 2003 May;139(1):163-71. doi: 10.1038/sj.bjp.0705232.
Ref 66 A novel peroxisome proliferator-activated receptor alpha/gamma dual agonist demonstrates favorable effects on lipid homeostasis. Endocrinology. 2004 Apr;145(4):1640-8. doi: 10.1210/en.2003-1270. Epub 2003 Dec 30.
Ref 67 Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation. J Med Chem. 2009 Aug 13;52(15):4631-9. doi: 10.1021/jm900326c.
Ref 68 Pharmacological profiles of a novel oral antidiabetic agent, JTT-501, an isoxazolidinedione derivative. Eur J Pharmacol. 1999 Jan 8;364(2-3):211-9. doi: 10.1016/s0014-2999(98)00832-2.
Ref 69 Antidiabetic and hypolipidemic potential of DRF 2519--a dual activator of PPAR-alpha and PPAR-gamma. Eur J Pharmacol. 2004 May 3;491(2-3):195-206. doi: 10.1016/j.ejphar.2004.03.034.
Ref 70 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
Ref 71 Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists. J Med Chem. 2004 May 6;47(10):2422-5. doi: 10.1021/jm0342616.
Ref 72 CN patent application no. 102459215, 3-(4-aminophenyl)-2-furancarboxylic acid derivative and pharmaceutically acceptable salt thereof.
Ref 73 Phenylacetic acid derivatives as hPPAR agonists. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80. doi: 10.1016/s0960-894x(03)00115-x.
Ref 74 Oleoylethanolamide, an endogenous PPAR-alpha agonist, lowers body weight and hyperlipidemia in obese rats. Neuropharmacology. 2005 Jun;48(8):1147-53. doi: 10.1016/j.neuropharm.2005.02.013. Epub 2005 Apr 21.