Target Information

Target General Information

Target ID

T86591 (Former ID: TTDS00340)

Target Name

Peroxisome proliferator-activated receptor alpha (PPARA)

Synonyms

Peroxisome proliferater-activated receptor alpha; PPARalpha; PPAR-alpha; PPAR; Nuclear receptor subfamily 1 group C member 1; NR1C1

Gene Name

PPARA

Target Type

Successful target

[1]

Disease

[+] 3 Target-related Diseases

Hyper-lipoproteinaemia [ICD-11: 5C80]

Hyperlipidemia [ICD-11: 5C80]

Type 2 diabetes mellitus [ICD-11: 5A11]

Function

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 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. Ligand-activated transcription factor.

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BioChemical Class

Nuclear hormone receptor

UniProt ID

PPARA_HUMAN

Sequence

MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSC
PGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACE
GCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSE
KAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFV
IHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANL
DLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFD
FAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDI
FLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

HIT2.0 ID

T49ORJ

Drugs and Modes of Action

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Approved Drug(s)

[+] 5 Approved Drugs

Bezafibrate

Drug Info

Approved

Hyperlipidaemia

[2], [3]

Ciprofibrate

Drug Info

Approved

Hyperlipoproteinemia

[3], [4], [5]

Fenofibrate

Drug Info

Approved

High cholesterol level

[6], [7]

Lobeglitazone

Drug Info

Approved

Type-2 diabetes

[8]

Pemafibrate

Drug Info

Approved

Hyperlipidemia

[9]

Clinical Trial Drug(s)

[+] 16 Clinical Trial Drugs

CS-038

Drug Info

Phase 3

Type-2 diabetes

[10]

GFT-505

Drug Info

Phase 3

Non-alcoholic steatohepatitis

[11]

Imiglitazar

Drug Info

Phase 3

Type-2 diabetes

[12], [13]

Ragaglitazar

Drug Info

Phase 3

Type-1 diabetes

[14], [15]

TESAGLITAZAR

Drug Info

Phase 3

Type-1 diabetes

[16]

ZYH-1

Drug Info

Phase 3

Lipid metabolism disorder

[17]

GFT14

Drug Info

Phase 2

Hyperlipidaemia

[18]

LY-518674

Drug Info

Phase 2

Diabetic complication

[19], [20]

Naveglitazar

Drug Info

Phase 2

Diabetic complication

[21]

ONO-5129

Drug Info

Phase 2

Diabetic complication

[22]

ZYH7

Drug Info

Phase 2

Lipid metabolism disorder

[23]

AVE0897

Drug Info

Phase 1

Type-2 diabetes

[24]

CDT-fenofibrate

Drug Info

Phase 1

Hyperlipidaemia

[25]

GW-409544

Drug Info

Phase 1

Hyperlipidaemia

[26], [27]

Oxeglitazar

Drug Info

Phase 1

Gout

[28]

TPST-1120

Drug Info

Phase 1

Solid tumour/cancer

[29]

Discontinued Drug(s)

[+] 22 Discontinued Drugs

Aleglitazar

Drug Info

Discontinued in Phase 3

Type-2 diabetes

[30], [31]

AVE-0847

Drug Info

Discontinued in Phase 2

Hyperlipidaemia

[32]

AVE-8134

Drug Info

Discontinued in Phase 2

Heart failure

[33]

BM-17.0744

Drug Info

Discontinued in Phase 2

Type-1 diabetes

[34]

GSK-677954

Drug Info

Discontinued in Phase 2

Non-alcoholic fatty liver disease

[35]

Indeglitazar

Drug Info

Discontinued in Phase 2

Type-2 diabetes

[36]

KRP-101

Drug Info

Discontinued in Phase 2

Hyperlipidaemia

[37]

KRP-297

Drug Info

Discontinued in Phase 2

Type-2 diabetes

[38]

NS-220

Drug Info

Discontinued in Phase 2

Hyperlipidaemia

[39], [40]

Reglixane

Drug Info

Discontinued in Phase 2

Diabetic complication

[41]

Sodelglitazar

Drug Info

Discontinued in Phase 2

Hyperlipidaemia

[42]

AR-H049020

Drug Info

Discontinued in Phase 1

Type-1 diabetes

[43]

DRF 10945

Drug Info

Discontinued in Phase 1

Hyperlipidaemia

[44]

E-3030

Drug Info

Discontinued in Phase 1

Hyperlipidaemia

[45]

LG-101280

Drug Info

Discontinued in Phase 1

Arteriosclerosis

[46]

LY-929

Drug Info

Discontinued in Phase 1

Lipid metabolism disorder

[47], [46]

MP-136

Drug Info

Discontinued in Phase 1

Lipid metabolism disorder

[48]

BVT-142

Drug Info

Terminated

Type-2 diabetes

[53]

CS-204

Drug Info

Terminated

Metabolic disorder

[54]

CS-207

Drug Info

Terminated

Cardiovascular disease

[55]

KRP-105

Drug Info

Terminated

Lipid metabolism disorder

[56]

Sipoglitazar

Drug Info

Terminated

Diabetic complication

[57]

Preclinical Drug(s)

[+] 4 Preclinical Drugs

MC-3001

Drug Info

Preclinical

Lipid metabolism disorder

[49]

MC-3002

Drug Info

Preclinical

Metabolic disorder

[50]

PIRINIXIC ACID

Drug Info

Preclinical

Pulmonary fibrosis

[51]

Romazarit

Drug Info

Preclinical

Rheumatoid arthritis

[52]

Mode of Action

[+] 5 Modes of Action

Agonist

[+] 43 Agonist drugs

Bezafibrate

Drug Info

[58]

Ciprofibrate

Drug Info

[1]

Fenofibrate

Drug Info

[1]

Lobeglitazone

Drug Info

[8]

Pemafibrate

Drug Info

[9]

GFT14

Drug Info

[66]

LY-518674

Drug Info

[67]

ZYH7

Drug Info

[70]

AVE0897

Drug Info

[71]

CDT-fenofibrate

Drug Info

[25]

Flavonoid derivative 8

Drug Info

[73]

PMID25416646-Compound-Figure5-A

Drug Info

[73]

PMID25416646-Compound-Figure5-H

Drug Info

[73]

Aleglitazar

Drug Info

[74]

AVE-8134

Drug Info

[76]

GSK-677954

Drug Info

[35]

Indeglitazar

Drug Info

[78]

KRP-101

Drug Info

[79], [80]

NS-220

Drug Info

[5], [82]

Sodelglitazar

Drug Info

[83]

AR-H049020

Drug Info

[84]

DRF 10945

Drug Info

[85]

LY-929

Drug Info

[88]

MP-136

Drug Info

[89]

MC-3001

Drug Info

[90]

BVT-142

Drug Info

[53], [93]

CS-204

Drug Info

[94]

CS-207

Drug Info

[95]

KRP-105

Drug Info

[96]

(E)-4-(3,5-dimethoxystyryl)phenol

Drug Info

[89]

8S-HETE

Drug Info

[98]

AD-5061

Drug Info

[62]

CP-775146

Drug Info

[100]

DB-900

Drug Info

[101]

DRF 2519

Drug Info

[103]

eicosatetranoic acid

Drug Info

[104]

Fibrates

Drug Info

[7]

GW7647

Drug Info

[107]

LY-465608

Drug Info

[109]

N-oleoylethanolamide

Drug Info

[110]

pristanic acid

Drug Info

[111]

reglitazar

Drug Info

[112]

TZD18

Drug Info

[113]

Modulator

[+] 22 Modulator drugs

CS-038

Drug Info

[59], [60]

GFT-505

Drug Info

[61]

Imiglitazar

Drug Info

[62], [63]

MURAGLITAZAR

Drug Info

[64]

Ragaglitazar

Drug Info

[15]

TESAGLITAZAR

Drug Info

[65]

ZYH-1

Drug Info

[57]

Naveglitazar

Drug Info

[68]

ONO-5129

Drug Info

[69]

GW-409544

Drug Info

[27]

Oxeglitazar

Drug Info

[28]

AVE-0847

Drug Info

[75]

KRP-297

Drug Info

[81]

Reglixane

Drug Info

[69]

E-3030

Drug Info

[86]

LG-101280

Drug Info

[87]

MC-3002

Drug Info

[69]

Romazarit

Drug Info

[92]

Sipoglitazar

Drug Info

[57]

GW-2331

Drug Info

[106]

LL-6531

Drug Info

[89]

ZY H2

Drug Info

[114]

Antagonist

[+] 1 Antagonist drugs

TPST-1120

Drug Info

[72]

Activator

[+] 1 Activator drugs

BM-17.0744

Drug Info

[5], [77]

Inhibitor

[+] 9 Inhibitor drugs

PIRINIXIC ACID

Drug Info

[91]

(9Z,12E)-12-nitrooctadeca-9,12-dienoic acid

Drug Info

[97]

(E)-12-Nitrooctadec-12-enoic Acid

Drug Info

[97]

(E)-13-Nitrooctadec-12-enoic Acid

Drug Info

[97]

BMS-687453

Drug Info

[99]

Deoxy-Bigchap

Drug Info

[102]

GSK-9578

Drug Info

[1], [105]

L-165461

Drug Info

[108]

L-796449

Drug Info

[108]

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

Top

Target-regulating microRNAs

Target-regulating microRNAs Info

Target-interacting Proteins

Target-interacting Proteins Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways		Top
KEGG Pathway	[+] 6 KEGG Pathways	+
1	PPAR signaling pathway
2	cAMP signaling pathway
3	Adipocytokine signaling pathway
4	Glucagon signaling pathway
5	Non-alcoholic fatty liver disease (NAFLD)
6	Hepatitis C
PID Pathway	[+] 1 PID Pathways	+
1	RXR and RAR heterodimerization with other nuclear receptor
Reactome	[+] 10 Reactome Pathways	+
1	RORA activates gene expression
2	BMAL1:CLOCK,NPAS2 activates circadian gene expression
3	PPARA activates gene expression
4	YAP1- and WWTR1 (TAZ)-stimulated gene expression
5	Transcriptional activation of mitochondrial biogenesis
6	Activation of gene expression by SREBF (SREBP)
7	Transcriptional regulation of white adipocyte differentiation
8	Nuclear Receptor transcription pathway
9	Regulation of lipid metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
10	Circadian Clock
WikiPathways	[+] 12 WikiPathways	+
1	Nuclear Receptors in Lipid Metabolism and Toxicity
2	Nuclear Receptors Meta-Pathway
3	Estrogen Receptor Pathway
4	PPAR Alpha Pathway
5	Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
6	Transcriptional Regulation of White Adipocyte Differentiation
7	YAP1- and WWTR1 (TAZ)-stimulated gene expression
8	Activation of Gene Expression by SREBP (SREBF)
9	Adipogenesis
10	SREBF and miR33 in cholesterol and lipid homeostasis
11	Circadian Clock
12	Nuclear Receptors

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

Target QSAR Model

References

Top

REF 1

Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42.

REF 2

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. (Ligand id: 2668).

REF 3

Antidiabetic action of bezafibrate in a large observational database. Diabetes Care. 2009 Apr;32(4):547-51.

REF 4

REF 5

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 6

REF 7

Emerging antidyslipidemic drugs. Expert Opin Emerg Drugs. 2008 Jun;13(2):363-81.

REF 8

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.

REF 9

Pemafibrate: First Global Approval. Drugs. 2017 Oct;77(16):1805-1810.

REF 10

ClinicalTrials.gov (NCT02173457) Study of Chiglitazar Compare With Sitagliptin in Type 2 Diabetes Patients. U.S. National Institutes of Health.

REF 11

ClinicalTrials.gov (NCT02704403) Phase 3 Study to Evaluate the Efficacy and Safety of Elafibranor Versus Placebo in Patients With Nonalcoholic Steatohepatitis (NASH) (RESOLVE-IT). U.S. National Institutes of Health.

REF 12

REF 13

Medicinal Chemistry and Actions of Dual and Pan PPAR Modulators. Open Med Chem J. 2011;5(Suppl 2):93-8.

REF 14

REF 15

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.

REF 16

ClinicalTrials.gov (NCT00229710) GALLEX 9: Safety and Tolerability of Oral Tesaglitazar When Added to Insulin Therapy in Patients With Type 2 Diabetes. U.S. National Institutes of Health.

REF 17

A multicenter, prospective, randomized, double-blind study to evaluate the safety and efficacy of Saroglitazar 2 and 4 g compared with placebo in type 2 diabetes mellitus patients having hypertriglyceridemia not controlled with atorvastatin therapy (PRESS VI). Diabetes Technol Ther. 2014 Feb;16(2):63-71.

REF 18

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 19

REF 20

ClinicalTrials.gov (NCT00327002) A Mechanistic Study of the Effects of LY518674 on High-Density Lipoprotein Cholesterol (HDL-C) Metabolism. U.S. National Institutes of Health.

REF 21

ClinicalTrials.gov (NCT00065312) An Evaluation of an Oral Antidiabetic Agent for the Treatment of Type 2 Diabetes. U.S. National Institutes of Health.

REF 22

ClinicalTrials.gov (NCT00335712) Pilot Study of ONO-5129 in Patients With Type 2 Diabetes Mellitus. U.S. National Institutes of Health.

REF 23

ClinicalTrials.gov (NCT01539616) A Clinical Trial to Evaluate the Safety and Efficacy of ZYH7 Compared to Fenofibrate in Patients With Dyslipidemia. U.S. National Institutes of Health.

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 800022196)

REF 25

Mechanism of action of fibrates on lipid and lipoprotein metabolism. Circulation. 1998 Nov 10;98(19):2088-93.

REF 26

REF 27

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.

REF 28

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.

REF 29

ClinicalTrials.gov (NCT03829436) TPST-1120 as Monotherapy and in Combination With Nivolumab in Subjects With Advanced Cancers. U.S. National Institutes of Health.

REF 30

REF 31

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017317)

REF 32

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020608)

REF 33

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021122)

REF 34

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011739)

REF 35

Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58.

REF 36

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022483)

REF 37

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018628)

REF 38

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010490)

REF 39

REF 40

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017798)

REF 41

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008953)

REF 42

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018093)

REF 43

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016001)

REF 44

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020522)

REF 45

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021476)

REF 46

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014823)

REF 47

REF 48

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031057)

REF 49

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 50

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021065)

REF 51

Targeting metabolic dysregulation for fibrosis therapy. Nat Rev Drug Discov. 2020 Jan;19(1):57-75.

REF 52

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000969)

REF 53

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.

REF 54

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026847)

REF 55

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 56

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026674)

REF 57

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.

REF 58

Bezafibrate at clinically relevant doses decreases serum/liver triglycerides via down-regulation of sterol regulatory element-binding protein-1c in... Mol Pharmacol. 2009 Apr;75(4):782-92.

REF 59

Determination of chiglitazar, a dual alpha/gamma peroxisome proliferator-activated receptor (PPAR) agonist, in human plasma by liquid chromatograph... Pharmazie. 2007 Nov;62(11):825-9.

REF 60

The PPARalpha/gamma dual agonist chiglitazar improves insulin resistance and dyslipidemia in MSG obese rats.Br J Pharmacol.2006 Jul;148(5):610-8.

REF 61

Dual peroxisome proliferator-activated receptor / agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects.Diabetes Care.2013 Oct;36(10):2923-30.

REF 62

A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. Eur J Pharmacol. 2004 Jul 8;495(1):17-26.

REF 63

A potent activator of PPARalpha and gamma reduces the vascular cell recruitment and inhibits the intimal thickning in hypercholesterolemic rabbits. Atherosclerosis. 2005 Jan;178(1):1-7.

REF 64

Muraglitazar, a dual (alpha/gamma) PPAR activator: a randomized, double-blind, placebo-controlled, 24-week monotherapy trial in adult patients with... Clin Ther. 2005 Aug;27(8):1181-95.

REF 65

Tesaglitazar, a dual PPAR-/ agonist, hamster carcinogenicity, investigative animal and clinical studies.Toxicol Pathol.2012;40(1):18-32.

REF 66

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 67

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.

REF 68

The disposition and metabolism of naveglitazar, a peroxisome proliferator-activated receptor alpha-gamma dual, gamma-dominant agonist in mice, rats... Drug Metab Dispos. 2007 Jan;35(1):51-61.

REF 69

Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

REF 70

Clinical pipeline report, company report or official report of Zydus Cadila.

REF 71

Pharma & Vaccines. Product Development Pipeline. April 29 2009.

REF 72

Clinical pipeline report, company report or official report of Tempest Therapeutics.

REF 73

PPAR ligands and their therapeutic applications: a patent review (2008 - 2014).Expert Opin Ther Pat. 2015 Feb;25(2):175-91.

REF 74

Clinical pipeline report, company report or official report of Roche (2009).

REF 75

DOI: 10.1038/scibx.2012.669

REF 76

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.

REF 77

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.

REF 78

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.

REF 79

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.

REF 80

A novel PPARalpha agonist ameliorates insulin resistance in dogs fed a high-fat diet. Am J Physiol Endocrinol Metab. 2008 May;294(5):E833-40.

REF 81

KRP-297, MCC-555. Nihon Rinsho. 2001 Nov;59(11):2200-6.

REF 82

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.

REF 83

Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar. Protein Pept Lett. 2011 Oct;18(10):1021-7.

REF 84

CN patent application no. 100577175, Combination therapy comprising glucose reabsorption inhibitors and PPAR modulators.

REF 85

Peroxisome proliferator-activated receptors, metabolic syndrome and cardiovascular disease. Future Cardiol. 2010 September; 6(5): 657-691.

REF 86

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.

REF 87

A peroxisome proliferator-activated receptor alpha/gamma dual agonist with a unique in vitro profile and potent glucose and lipid effects in rodent... Mol Endocrinol. 2005 Jun;19(6):1593-605.

REF 88

CN patent application no. 1882326, Ppar agonists for the treatment of hcv infection.

REF 89

REF 90

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 91

O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3185-90.

REF 92

Fibrates as therapy for osteoarthritis and rheumatoid arthritis A systematic review. Ther Adv Musculoskelet Dis. 2013 February; 5(1): 33-44.

REF 93

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