Target Information

Target General Information

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Target ID

T58921 (Former ID: TTDS00338)

Target Name

Peroxisome proliferator-activated receptor gamma (PPAR-gamma)

Synonyms

PPAR-gamma; Nuclear receptor subfamily 1 group C member 3; NR1C3

Gene Name

PPARG

Target Type

Successful target

[1]

Disease

[+] 3 Target-related Diseases

Acute diabete complication [ICD-11: 5A2Y]

Alzheimer disease [ICD-11: 8A20]

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

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 proinflammatory responses. Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of ARNTL/BMAL1 in the blood vessels (By similarity).

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BioChemical Class

Nuclear hormone receptor

UniProt ID

PPARG_HUMAN

Sequence

MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF
DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT
QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC
RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR
ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE
QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS
LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII
LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL
LQVIKKTETDMSLHPLLQEIYKDLY

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3D Structure

Click to Show 3D Structure of This Target

PDB

ADReCS ID

BADD_A02556 ; BADD_A04820 ; BADD_A05675

HIT2.0 ID

T58J2Y

Drugs and Modes of Action

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Approved Drug(s)

[+] 5 Approved Drugs

Lobeglitazone

Drug Info

Approved

Type-2 diabetes

[2]

Pioglitazone

Drug Info

Approved

Diabetic complication

[3], [4]

Rosiglitazone XR

Drug Info

Approved

Type-2 diabetes

[5]

Thiazolidinedione

Drug Info

Approved

Alzheimer disease

[6]

Troglitazone

Drug Info

Approved

Diabetic complication

[7], [8]

Clinical Trial Drug(s)

[+] 25 Clinical Trial Drugs

Balaglitazone

Drug Info

Phase 3

Type-1 diabetes

[9]

CS-038

Drug Info

Phase 3

Type-2 diabetes

[10]

FARGLITAZAR

Drug Info

Phase 3

Type-1 diabetes

[11], [12]

Imiglitazar

Drug Info

Phase 3

Type-2 diabetes

[13], [14]

Ragaglitazar

Drug Info

Phase 3

Type-1 diabetes

[15], [16]

Rivoglitazone

Drug Info

Phase 3

Ocular inflammation

[17]

Rosiglitazone + metformin

Drug Info

Phase 3

Diabetic complication

[18]

Rosiglitazone + simvastatin

Drug Info

Phase 3

Type-2 diabetes

[19]

TESAGLITAZAR

Drug Info

Phase 3

Type-1 diabetes

[20]

ZYH-1

Drug Info

Phase 3

Lipid metabolism disorder

[21]

MBX-102

Drug Info

Phase 2/3

Gout

[22]

CHS-131

Drug Info

Phase 2

Multiple sclerosis

[23]

FK-614

Drug Info

Phase 2

Type-2 diabetes

[24]

GED-0507-34-Levo

Drug Info

Phase 2

Inflammatory bowel disease

[25]

MBX-2044

Drug Info

Phase 2

Type-2 diabetes

[26]

Naveglitazar

Drug Info

Phase 2

Diabetic complication

[27]

Netoglitazone

Drug Info

Phase 2

Non-alcoholic fatty liver disease

[28], [29]

OMS405

Drug Info

Phase 2

Nicotine dependence

[30]

ONO-5129

Drug Info

Phase 2

Diabetic complication

[31]

T3D-959

Drug Info

Phase 1/2

Alzheimer disease

[32]

CLX-0921

Drug Info

Phase 1

Type-2 diabetes

[33]

DSP-8658

Drug Info

Phase 1

Type-2 diabetes

[34]

Englitazone sodium

Drug Info

Phase 1

Type-2 diabetes

[35]

GW-409544

Drug Info

Phase 1

Hyperlipidaemia

[36], [37]

Oxeglitazar

Drug Info

Phase 1

Gout

[38]

Discontinued Drug(s)

[+] 18 Discontinued Drugs

AVE-0847

Drug Info

Discontinued in Phase 2

Hyperlipidaemia

[39]

GSK-677954

Drug Info

Discontinued in Phase 2

Non-alcoholic fatty liver disease

[29]

Indeglitazar

Drug Info

Discontinued in Phase 2

Type-2 diabetes

[40]

KRP-297

Drug Info

Discontinued in Phase 2

Type-2 diabetes

[41]

Reglixane

Drug Info

Discontinued in Phase 2

Diabetic complication

[42]

Sodelglitazar

Drug Info

Discontinued in Phase 2

Hyperlipidaemia

[43]

YM-440

Drug Info

Discontinued in Phase 2

Type-1 diabetes

[44]

DS-6930

Drug Info

Discontinued in Phase 1

Diabetic complication

[45]

E-3030

Drug Info

Discontinued in Phase 1

Hyperlipidaemia

[46]

LY-929

Drug Info

Discontinued in Phase 1

Lipid metabolism disorder

[47], [48]

AD-5075

Drug Info

Terminated

Type-2 diabetes

[51], [52]

AKP-320

Drug Info

Terminated

Type-2 diabetes

[53]

BVT-142

Drug Info

Terminated

Type-2 diabetes

[54]

CS-204

Drug Info

Terminated

Metabolic disorder

[55]

DARGLITAZONE

Drug Info

Terminated

Diabetic complication

[56]

Edaglitazone

Drug Info

Terminated

Type-2 diabetes

[57]

SB-219994

Drug Info

Terminated

Diabetic complication

[58], [59]

Sipoglitazar

Drug Info

Terminated

Diabetic complication

[60]

Preclinical Drug(s)

[+] 2 Preclinical Drugs

Ciglitazone

Drug Info

Preclinical

Pulmonary fibrosis

[49]

MC-3002

Drug Info

Preclinical

Metabolic disorder

[50]

Mode of Action

[+] 4 Modes of Action

Agonist

[+] 51 Agonist drugs

Lobeglitazone

Drug Info

[2]

Pioglitazone

Drug Info

[1], [61]

Rosiglitazone XR

Drug Info

[62]

Thiazolidinedione

Drug Info

[1]

Troglitazone

Drug Info

[1], [63], [64]

Glitazone

Drug Info

[65]

Rivoglitazone

Drug Info

[74]

Rosiglitazone + metformin

Drug Info

[62]

Rosiglitazone + simvastatin

Drug Info

[62]

MBX-102

Drug Info

[26]

FK-614

Drug Info

[24]

GED-0507-34-Levo

Drug Info

[76]

MBX-2044

Drug Info

[26]

OMS405

Drug Info

[79]

CLX-0921

Drug Info

[33]

Englitazone sodium

Drug Info

[35], [83]

1-(biphenyl-4-yl-methyl)-1H-imidazole derivative 1

Drug Info

[84]

3-phenyl acrylic acid derivative 1

Drug Info

[84]

A-substituted phenylpropionic acid derivative 1

Drug Info

[84]

A-substituted phenylpropionic acid derivative 2

Drug Info

[84]

Biaromatic compound 1

Drug Info

[84]

Crystalline anhydrous toluene derivative 1

Drug Info

[84]

Flavonoid derivative 8

Drug Info

[84]

Fused aromatic compound 1

Drug Info

[84]

Fused ring compound 1

Drug Info

[84]

MRL20

Drug Info

[84]

MRL24

Drug Info

[84]

Phenylpropionic acid derivative 1

Drug Info

[84]

Phenylpyridine derivative 3

Drug Info

[84]

PMID25416646-Compound-Figure2-J

Drug Info

[84]

PMID25416646-Compound-Figure2-K

Drug Info

[84]

PMID25416646-Compound-Figure2-N

Drug Info

[84]

PMID25416646-Compound-Figure5-A

Drug Info

[84]

PMID25416646-Compound-Figure5-C

Drug Info

[84]

PMID25416646-Compound-Figure5-E

Drug Info

[84]

PMID25416646-Compound-Figure5-H

Drug Info

[84]

Spirolaxine derivative 1

Drug Info

[84]

Sulfonamide derivative 18

Drug Info

[84]

Thiazolidine dione crystalline derivative 1

Drug Info

[84]

GSK-677954

Drug Info

[29]

Indeglitazar

Drug Info

[86]

Sodelglitazar

Drug Info

[88]

LY-929

Drug Info

[92]

Ciglitazone

Drug Info

[93]

BVT-142

Drug Info

[54], [95]

CS-204

Drug Info

[96]

DARGLITAZONE

Drug Info

[97], [83]

SB-219994

Drug Info

[98]

15-deoxy-Delta(12, 14)-prostaglandin J(2)

Drug Info

[63]

DB-900

Drug Info

[100]

GW7845

Drug Info

[102]

Modulator

[+] 28 Modulator drugs

Balaglitazone

Drug Info

[66]

CS-038

Drug Info

[67], [68]

FARGLITAZAR

Drug Info

[69], [70]

Imiglitazar

Drug Info

[71], [72]

MURAGLITAZAR

Drug Info

[73]

Ragaglitazar

Drug Info

[16]

TESAGLITAZAR

Drug Info

[75]

ZYH-1

Drug Info

[60]

CHS-131

Drug Info

[23]

Naveglitazar

Drug Info

[77]

Netoglitazone

Drug Info

[78]

ONO-5129

Drug Info

[80]

T3D-959

Drug Info

[81]

DSP-8658

Drug Info

[82]

GW-409544

Drug Info

[37]

Oxeglitazar

Drug Info

[38]

AVE-0847

Drug Info

[85]

KRP-297

Drug Info

[87]

Reglixane

Drug Info

[80]

DS-6930

Drug Info

[90]

E-3030

Drug Info

[91]

MC-3002

Drug Info

[80]

AD-5075

Drug Info

[52]

AKP-320

Drug Info

[94]

Edaglitazone

Drug Info

[57]

Sipoglitazar

Drug Info

[60]

GW-2331

Drug Info

[101]

ZY H2

Drug Info

[103]

Ligand

[+] 1 Ligand drugs

Cannabinoid quinone derivative 1

Drug Info

[84]

Inhibitor

[+] 8 Inhibitor drugs

YM-440

Drug Info

[89], [83]

(2S)-2-(4-chlorophenoxy)-3-phenylpropanoic acid

Drug Info

[99]

(2S)-2-(4-ethylphenoxy)-3-phenylpropanoic acid

Drug Info

[99]

(2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid

Drug Info

[99]

(9Z,11E,13S)-13-hydroxyoctadeca-9,11-dienoic acid

Drug Info

[99]

2-chloro-5-nitro-N-phenylbenzamide

Drug Info

[99]

3-(5-methoxy-1H-indol-3-yl)propanoic acid

Drug Info

[99]

9-hydroxyoctadecadienoic acid

Drug Info

[99]

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(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

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

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Target-regulating microRNAs

Target-regulating microRNAs Info

Target-interacting Proteins

Target-interacting Proteins Info

Target Profiles in Patients

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Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

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KEGG Pathway

[+] 7 KEGG Pathways

PPAR signaling pathway

AMPK signaling pathway

Osteoclast differentiation

Huntington's disease

Pathways in cancer

Transcriptional misregulation in cancer

Thyroid cancer

NetPath Pathway

[+] 3 NetPath Pathways

IL1 Signaling Pathway

TGF_beta_Receptor Signaling Pathway

Leptin Signaling Pathway

Panther Pathway

[+] 1 Panther Pathways

CCKR signaling map ST

PID Pathway

[+] 5 PID Pathways

Noncanonical Wnt signaling pathway

Calcineurin-regulated NFAT-dependent transcription in lymphocytes

Signaling events mediated by HDAC Class I

RXR and RAR heterodimerization with other nuclear receptor

Regulation of retinoblastoma protein

Reactome

[+] 3 Reactome Pathways

PPARA activates gene expression

Transcriptional regulation of white adipocyte differentiation

Nuclear Receptor transcription pathway

WikiPathways

[+] 8 WikiPathways

Wnt Signaling Pathway Netpath

Nuclear Receptors in Lipid Metabolism and Toxicity

Differentiation of white and brown adipocyte

Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)

Transcriptional Regulation of White Adipocyte Differentiation

Adipogenesis

SREBP signalling

Nuclear Receptors

Target-Related Models and Studies

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Target Validation

Target Validation Info

Target QSAR Model

References

Top

REF 1

Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7.

REF 2

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 3

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: 2694).

REF 4

Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes. Curr Drug Targets. 2009 Jan;10(1):71-87.

REF 5

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

REF 6

Thiazolidinediones: a comparative review of approved uses. Diabetes Technol Ther. 2000 Autumn;2(3):429-40.

REF 7

REF 8

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 9

ClinicalTrials.gov (NCT00515632) Efficacy and Safety of Treatment With Balaglitazone in Type 2 Diabetes Patients on Stable Insulin Therapy. U.S. National Institutes of Health.

REF 10

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

REF 11

REF 12

Clinical pipeline report, company report or official report of MacroGenics.

REF 13

REF 14

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

REF 15

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.

REF 17

ClinicalTrials.gov (NCT00571519) Randomized, Double-blind, Active-controlled, Study of Rivoglitazone in Type 2 Diabetes Mellitus. U.S. National Institutes of Health.

REF 18

ClinicalTrials.gov (NCT00499707) Efficacy and Safety Study of Rosiglitazone/Metformin Therapy vs Rosiglitazone and Metformin in Type 2 Diabetes Subjects. U.S. National Institutes of Health.

REF 19

Clinical pipeline report, company report or official report of GlaxoSmithKline.

REF 20

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 21

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 22

ClinicalTrials.gov (NCT00353587) Safety and Efficacy Study of Metaglidasen in Type 2 Diabetes in Patients Suboptimally Controlled on Insulin. U.S. National Institutes of Health.

REF 23

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 24

FK-614, a selective peroxisome proliferator-activated receptor gamma agonist, improves peripheral glucose utilization while decreasing hepatic insulin extraction in alloxan-induced diabetic dogs. Metabolism. 2005 Sep;54(9):1250-8.

REF 25

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032997)

REF 26

MBX-102/JNJ39659100, a novel peroxisome proliferator-activated receptor-ligand with weak transactivation activity retains antidiabetic properties in the absence of weight gain and edema. Mol Endocrinol. 2009 Jul;23(7):975-88.

REF 27

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

REF 28

REF 29

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

REF 30

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035962)

REF 31

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

REF 32

ClinicalTrials.gov (NCT02560753) Feasibility Study in Subjects With Mild to Moderate Alzheimer's Disease.

REF 33

A novel peroxisome proliferator-activated gamma (PPAR gamma) agonist, CLX-0921, has potent antihyperglycemic activity with low adipogenic potential. Metabolism. 2003 Aug;52(8):1012-8.

REF 34

ClinicalTrials.gov (NCT01042106) Safety, Pharmacokinetics and Pharmacodynamics of DSP-8658 in Patients With Type 2 Diabetes Mellitus and Healthy Adults. U.S. National Institutes of Health.

REF 35

PPARgamma agonists in the treatment of type II diabetes: is increased fatness commensurate with long-term efficacy. Int J Obes Relat Metab Disord. 2003 Feb;27(2):147-61.

REF 36

REF 37

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 38

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 39

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 40

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 41

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 42

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 43

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 44

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010082)

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 800036558)

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 800021476)

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 800014823)

REF 49

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

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

REF 52

Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-gamma: binding and activation correlate with antidiabetic actions in db/db mice. Endocrinology. 1996 Oct;137(10):4189-95.

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 800022081)

REF 54

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 55

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 56

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003002)

REF 57

A specific peroxisome proliferator-activated receptor-gamma (PPAR-gamma) ligand, pioglitazone, ameliorates gastric mucosal damage induced by ischemia and reperfusion in rats. Redox Rep. 2002;7(5):343-6.

REF 58

REF 59

Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma. J Pharmacol Exp Ther. 1998 Feb;284(2):751-9.

REF 60

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 61

Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.

REF 62

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

REF 63

Expression of peroxisome proliferator-activated receptors (PPARs) in human urinary bladder carcinoma and growth inhibition by its agonists. Int J Cancer. 2003 May 1;104(5):597-602.

REF 64

Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.

REF 65

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

REF 66

Balaglitazone: a second generation peroxisome proliferator-activated receptor (PPAR) gamma () agonist.Mini Rev Med Chem.2012 Feb;12(2):87-97.

REF 67

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 68

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 69

Rosiglitazone (BRL49653), a PPARgamma-selective agonist, causes peroxisome proliferator-like liver effects in obese mice. J Lipid Res. 1999 Jul;40(7):1177-84.

REF 70

Rosiglitazone, an agonist of peroxisome proliferator-activated receptor gamma, reduces pulmonary inflammatory response in a rat model of endotoxemia. Inflamm Res. 2005 Nov;54(11):464-70.

REF 71

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 72

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 73

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 74

A randomized-controlled trial to investigate the effects of rivoglitazone, a novel PPAR gamma agonist on glucose-lipid control in type 2 diabetes. Diabetes Obes Metab. 2011 Sep;13(9):806-13.

REF 75

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

REF 76

PPAR-gamma in ulcerative colitis: a novel target for intervention. Curr Drug Targets. 2013 Nov;14(12):1501-7.

REF 77

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 78

Netoglitazone is a PPAR-gamma ligand with selective effects on bone and fat. Bone. 2006 Jan;38(1):74-84.

REF 79

Clinical pipeline report, company report or official report of Avarx.

REF 80

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

REF 81

Phrma report (2013 Alzheimers disease)

REF 82

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