Target Information

Target General Infomation
Target ID
T58921
Former ID
TTDS00338
Target Name
Peroxisome proliferator activated receptor gamma
Gene Name
PPARG
Synonyms
PPAR-gamma; PPARgamma; Transcription factor PPAR gamma receptor; PPARG
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Alzheimer disease; Type 2 diabetes [ICD9:331, 250; ICD10: G30, E11]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Drug abuse [ICD9: 303-304; ICD10: F10-F19]
Endometriosis [ICD9: 617; ICD10: N80]
Gout [ICD9: 274.00274.1274.8274.9; ICD10: M10]
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Lipid metabolism disorder [ICD10: E75-E78]
Metabolic disorders [ICD9: 270-279; ICD10: E70-E89]
Non-alcoholic fatty liver disease [ICD9: 571.8; ICD10: K76.0]
Nicotine dependence [ICD9: 305.1; ICD10: F17]
Ocular inflammation [ICD9: 370.33; ICD10: H16.229]
Obesity [ICD9: 278; ICD10: E66]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Type 1 diabetes [ICD9: 250; ICD10: E10]
Unspecified [ICD code not available]
Function
Receptor that bind peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-coa oxidase and activates its transcription.
BioChemical Class
Nuclear hormone receptor
Target Validation
T58921
UniProt ID
P37231
Sequence
MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF
DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT
QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC
RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR
ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE
QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS
LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII
LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL
LQVIKKTETDMSLHPLLQEIYKDLY
Drugs and Mode of Action
Drug(s) Pioglitazone Drug Info Approved Diabetes [1], [2]
Rosiglitazone XR Drug Info Approved Type 2 diabetes [3]
Thiazolidinedione Drug Info Approved Alzheimer disease [4]
Troglitazone Drug Info Approved Diabetes [5], [6]
Glitazone Drug Info Phase 4 Discovery agent [7]
Balaglitazone Drug Info Phase 3 Type 1 diabetes [8]
CS-038 Drug Info Phase 3 Type 2 diabetes [9]
FARGLITAZAR Drug Info Phase 3 Type 1 diabetes [10], [11]
Imiglitazar Drug Info Phase 3 Type 2 diabetes [12], [13]
Lobeglitazone Drug Info Phase 3 Diabetes [14]
MURAGLITAZAR Drug Info Phase 3 Discovery agent [15]
Ragaglitazar Drug Info Phase 3 Type 1 diabetes [16], [17]
Rivoglitazone Drug Info Phase 3 Ocular inflammation [18]
Rosiglitazone + metformin Drug Info Phase 3 Diabetes [19]
Rosiglitazone + simvastatin Drug Info Phase 3 Type 2 diabetes [20]
Rosiglitazone XR Drug Info Phase 3 Alzheimer disease [21]
TESAGLITAZAR Drug Info Phase 3 Type 1 diabetes [22]
ZYH-1 Drug Info Phase 3 Lipid metabolism disorder [23]
MBX-102 Drug Info Phase 2/3 Gout [24]
FK-614 Drug Info Phase 2 Type 2 diabetes [25]
GED-0507-34-Levo Drug Info Phase 2 Inflammatory bowel disease [26]
MBX-2044 Drug Info Phase 2 Type 2 diabetes [27]
Naveglitazar Drug Info Phase 2 Diabetes [28]
Netoglitazone Drug Info Phase 2 Non-alcoholic fatty liver disease [29], [30]
OMS405 Drug Info Phase 2 Nicotine dependence [31]
ONO-5129 Drug Info Phase 2 Diabetes [32]
Research programme: peroxisome proliferator-activated receptor gamma agonist, Omeros Drug Info Phase 2 Drug abuse [33]
T3D-959 Drug Info Phase 1/2 Alzheimer disease [34]
CLX-0921 Drug Info Phase 1 Type 2 diabetes [35]
DSP-8658 Drug Info Phase 1 Alzheimer disease; Type 2 diabetes [36]
Englitazone sodium Drug Info Phase 1 Type 2 diabetes [37]
GW-409544 Drug Info Phase 1 Hyperlipidaemia [38], [39]
Oxeglitazar Drug Info Phase 1 Gout [40]
MC-3002 Drug Info Preclinical Metabolic disorders [41]
AVE-0847 Drug Info Discontinued in Phase 2 Hyperlipidaemia [42]
Ciglitazone Drug Info Discontinued in Phase 2 Endometriosis [43], [44]
GSK-677954 Drug Info Discontinued in Phase 2 Non-alcoholic fatty liver disease [29]
Indeglitazar Drug Info Discontinued in Phase 2 Type 2 diabetes [45]
MK-767 (KRP-297) Drug Info Discontinued in Phase 2 Type 2 diabetes [46]
Reglixane Drug Info Discontinued in Phase 2 Diabetes [47]
Sodelglitazar Drug Info Discontinued in Phase 2 Hyperlipidaemia [48]
YM-440 Drug Info Discontinued in Phase 2 Type 1 diabetes [49]
DS-6930 Drug Info Discontinued in Phase 1 Diabetes [50]
E-3030 Drug Info Discontinued in Phase 1 Hyperlipidaemia [51]
LY-929 Drug Info Discontinued in Phase 1 Lipid metabolism disorder [52], [53]
AD-5075 Drug Info Terminated Type 2 diabetes [54], [55]
AKP-320 Drug Info Terminated Type 2 diabetes [56]
BVT-142 Drug Info Terminated Type 2 diabetes [57]
CS-204 Drug Info Terminated Metabolic disorders [58]
DARGLITAZONE Drug Info Terminated Diabetes [59]
Edaglitazone Drug Info Terminated Type 2 diabetes [60]
KRP-297 Drug Info Terminated Hyperlipidaemia [61], [62]
SB-219994 Drug Info Terminated Diabetes [63], [64]
Sipoglitazar Drug Info Terminated Diabetes [65]
Rosiglitazone XR Drug Info Investigative Discovery agent [66]
Inhibitor (2S)-2-(4-chlorophenoxy)-3-phenylpropanoic acid Drug Info [67]
(2S)-2-(4-ethylphenoxy)-3-phenylpropanoic acid Drug Info [67]
(2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid Drug Info [67]
(9S,10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid Drug Info [67]
(9Z,11E,13S)-13-hydroxyoctadeca-9,11-dienoic acid Drug Info [67]
2-chloro-5-nitro-N-phenylbenzamide Drug Info [67]
3-(5-methoxy-1H-indol-3-yl)propanoic acid Drug Info [67]
YM-440 Drug Info [68], [69]
Agonist 15-deoxy-Delta(12, 14)-prostaglandin J(2) Drug Info [70]
BVT-142 Drug Info [57], [71]
Ciglitazone Drug Info [72]
CLX-0921 Drug Info [35]
CS-204 Drug Info [73]
DARGLITAZONE Drug Info [74], [69]
DB-900 Drug Info [75]
Englitazone sodium Drug Info [37], [69]
FK-614 Drug Info [25]
GED-0507-34-Levo Drug Info [76]
Glitazone Drug Info [77]
GSK-677954 Drug Info [29]
GW7845 Drug Info [78]
Indeglitazar Drug Info [79]
Lobeglitazone Drug Info [14]
LY-929 Drug Info [80]
MBX-102 Drug Info [27]
MBX-2044 Drug Info [27]
OMS405 Drug Info [81]
Pioglitazone Drug Info [82]
Research programme: peroxisome proliferator-activated receptor gamma agonist, Omeros Drug Info [83]
Rivoglitazone Drug Info [84]
Rosiglitazone + metformin Drug Info [66]
Rosiglitazone + simvastatin Drug Info [66]
Rosiglitazone XR Drug Info [66]
SB-219994 Drug Info [85]
Sodelglitazar Drug Info [86]
Thiazolidinedione Drug Info [82]
Troglitazone Drug Info [82], [87], [70]
Modulator AD-5075 Drug Info [54]
AKP-320 Drug Info [88]
AVE-0847 Drug Info
Balaglitazone Drug Info
CS-038 Drug Info
DS-6930 Drug Info [89]
DSP-8658 Drug Info [90]
E-3030 Drug Info
Edaglitazone Drug Info [60]
FARGLITAZAR Drug Info
GW-2331 Drug Info
GW-409544 Drug Info [38]
Imiglitazar Drug Info [91]
KRP-297 Drug Info [61]
MC-3002 Drug Info [92]
MK-767 (KRP-297) Drug Info [93]
MURAGLITAZAR Drug Info
Naveglitazar Drug Info [94]
Netoglitazone Drug Info [95]
ONO-5129 Drug Info [92]
Oxeglitazar Drug Info [40]
Ragaglitazar Drug Info [16]
Reglixane Drug Info [92]
Sipoglitazar Drug Info [65]
T3D-959 Drug Info
TESAGLITAZAR Drug Info
ZY H2 Drug Info [96]
ZYH-1 Drug Info [65]
Binder PCG1 Drug Info [97]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway PPAR signaling pathway
AMPK signaling pathway
Osteoclast differentiation
Huntington&#039
s disease
Pathways in cancer
Transcriptional misregulation in cancer
Thyroid cancer
NetPath Pathway IL1 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
Leptin Signaling Pathway
PANTHER Pathway CCKR signaling map ST
Pathway Interaction Database 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 PPARA activates gene expression
Transcriptional regulation of white adipocyte differentiation
Nuclear Receptor transcription pathway
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
References
REF 1Emerging 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 2(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 3Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 4Thiazolidinediones: a comparative review of approved uses. Diabetes Technol Ther. 2000 Autumn;2(3):429-40.
REF 5Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
REF 6(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: 2693).
REF 7ClinicalTrials.gov (NCT00953498) Influence of Glitazones on the Vasodilatory Effect of High-density Lipoprotein (HDL) Lipoproteins. U.S. National Institutes of Health.
REF 8ClinicalTrials.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 9ClinicalTrials.gov (NCT02173457) Study of Chiglitazar Compare With Sitagliptin in Type 2 Diabetes Patients. U.S. National Institutes of Health.
REF 10(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: 2672).
REF 11Clinical pipeline report, company report or official report of MacroGenics.
REF 12Medicinal Chemistry and Actions of Dual and Pan PPAR Modulators. Open Med Chem J. 2011;5(Suppl 2):93-8.
REF 13(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: 2675).
REF 14Tolerability and pharmacokinetics of lobeglitazone (CKD-501), a peroxisome proliferator-activated receptor-gamma agonist: a single- and multiple-dose, double-blind, randomized control study in healthy male Korean subjects. Clin Ther. 2011 Nov;33(11):1819-30.
REF 15ClinicalTrials.gov (NCT00094991) Mechanism of Action and Efficacy of Muraglitazar in Type 2 Diabetes. U.S. National Institutes of Health.
REF 16Ragaglitazar: 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(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: 2664).
REF 18ClinicalTrials.gov (NCT00571519) Randomized, Double-blind, Active-controlled, Study of Rivoglitazone in Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
REF 19ClinicalTrials.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 20Clinical pipeline report, company report or official report of GlaxoSmithKline.
REF 21Rosiglitazone monotherapy in mild-to-moderate Alzheimer's disease: results from a randomized, double-blind, placebo-controlled phase III study. Dement Geriatr Cogn Disord. 2010;30(2):131-46.
REF 22ClinicalTrials.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 23A 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 24ClinicalTrials.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 25FK-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 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032997)
REF 27MBX-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 28ClinicalTrials.gov (NCT00065312) An Evaluation of an Oral Antidiabetic Agent for the Treatment of Type 2 Diabetes. U.S. National Institutes of Health.
REF 29Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58.
REF 30(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: 2707).
REF 31Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035962)
REF 32ClinicalTrials.gov (NCT00335712) Pilot Study of ONO-5129 in Patients With Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
REF 33Clinical pipeline report, company report or official report of Omeros Corp.
REF 34ClinicalTrials.gov (NCT02560753) Feasibility Study in Subjects With Mild to Moderate Alzheimer's Disease.
REF 35A 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 36ClinicalTrials.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 37PPARgamma 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 38Design 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 39(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: 3440).
REF 40Therapeutic 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 41Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021065)
REF 42Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020608)
REF 43(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: 2711).
REF 44Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004145)
REF 45Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022483)
REF 46Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010490)
REF 47Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008953)
REF 48Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018093)
REF 49Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010082)
REF 50Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036558)
REF 51Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021476)
REF 52(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: 2657).
REF 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014823)
REF 54Thiazolidinediones 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 55(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: 2701).
REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022081)
REF 57A 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. Epub 2004 Jul 15.
REF 58Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026847)
REF 59Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003002)
REF 60A 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 61KRP-297, MCC-555. Nihon Rinsho. 2001 Nov;59(11):2200-6.
REF 62(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: 2677).
REF 63Identification 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 64(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: 2698).
REF 65Pharmacokinetics, 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 66Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
REF 67The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 68The novel hypoglycemic agent YM440 improves hepatic insulin resistance in obese Zucker fatty rats. J Pharmacol Sci. 2006 Aug;101(4):311-7. Epub 2006 Aug 5.
REF 69Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 70Expression 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 71US patent application no. 7,816,328, Substituted fused heterocyclic c-glycosides.
REF 72New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202.
REF 73Peroxisome Proliferators-Activated Receptor (PPAR) Modulators and Metabolic Disorders. PPAR Res. 2008; 2008: 679137.
REF 74The PPAR-gamma agonist, darglitazone, restores acute inflammatory responses to cerebral hypoxia-ischemia in the diabetic ob/ob mouse. J Cereb Blood Flow Metab. 2010 February; 30(2): 352-360.
REF 75CN patent application no. 102459215, 3-(4-aminophenyl)-2-furancarboxylic acid derivative and pharmaceutically acceptable salt thereof.
REF 76PPAR-gamma in ulcerative colitis: a novel target for intervention. Curr Drug Targets. 2013 Nov;14(12):1501-7.
REF 77Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42.
REF 78A new ligand for the peroxisome proliferator-activated receptor-gamma (PPAR-gamma), GW7845, inhibits rat mammary carcinogenesis. Cancer Res. 1999 Nov 15;59(22):5671-3.
REF 79Scaffold-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 80CN patent application no. 1882326, Ppar agonists for the treatment of hcv infection.
REF 81Clinical pipeline report, company report or official report of Avarx.
REF 82Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7. Epub 2002 Oct 15.
REF 83Clinical pipeline report, company report or official report of omeros.
REF 84A 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 85PPAR-gamma agonists as therapy for diseases involving airway neutrophilia. Eur Respir J. 2004 Jul;24(1):18-23.
REF 86Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar. Protein Pept Lett. 2011 Oct;18(10):1021-7.
REF 87Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
REF 88Chronic glucose-lowering effects of rosiglitazone and bis(ethylmaltolato) oxovanadium(IV) in ZDF rats. Canadian Journal of Physiology and Pharmacology. 12/2003; 81(11):1049-55.
REF 89Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036558)
REF 90Effects of DSP-8658, a Novel Selective Peroxisome Proliferator-activated Receptors a/gamma Modulator, on Adipogenesis and Glucose Metabolism in Diabetic Obese Mice. Exp Clin Endocrinol Diabetes. 2015Sep;123(8):492-9.
REF 91A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. Eur J Pharmacol. 2004 Jul 8;495(1):17-26.
REF 92Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 93MK-767. Kyorin/Banyu/Merck. Curr Opin Investig Drugs. 2003 Apr;4(4):444-8.
REF 94The 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. Epub 2006 Sep 29.
REF 95Netoglitazone is a PPAR-gamma ligand with selective effects on bone and fat. Bone. 2006 Jan;38(1):74-84. Epub 2005 Aug 30.
REF 96The ChEMBL database in 2017.
REF 97Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.