Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

TTD Target ID: TTDS00338

Target Information
NamePeroxisome proliferator activated receptor gamma    
Type of targetSuccessful target    
SynonymsPPAR-gamma    
PPARgamma    
Transcription factor PPAR gamma receptor    
DiseaseAdrenocorticotrophic hormone-secreting pituitary tumors    [1]
Asthma    [2]
Atherosclerosis    [3]
Atopic dermatitis    [2]
Autoimmune diseases    [4]
Bladder cancer    [5]
Chronic inflammatory diseases    [6]
Crohn's disease, unspecified    [7]
Diabetes mellitus    [8]
Inflammation    [8]
Inflammatory bowel disease    [1]
Insulin resistance    [9]
Ischemic heart disease    [10]
Multiple sclerosis    [2]
Obesity    [11]
Pancreatic cancer    [12]
Psoriasis    [2]
Renal cell carcinoma    [13]
Testicular cancer    [14]
Thyroid follicular carcinoma    [15]
Ulcerative colitis    [7][2]
Drug(s)PioglitazoneApprovedDiabetes mellitus[16]
RosiglitazoneApprovedDiabetes mellitus[16]
TroglitazoneApprovedDiabetes mellitus[5][17][16]
Rosiglitazone & metforminPhase III completedType 2 diabetes ĘC extended release[18]
Rosiglitazone & simvastatinPhase III completedType 2 diabetes[18]
Rosiglitazone XRPhase IIIAlzheimer's disease[18]
GenisteinPhase IIProstate Cancer[19]
NetoglitazonePhase IINon-alcoholic fatty liver disease (NAFLD)[20]
GSK-677954Discontinued in Phase IINon-alcoholic fatty liver disease (NAFLD)[21]
BioChemical ClassZinc-finger    
UniProt IDP37231
PDB Structure1FM6; 1FM9; 1I7I; 1K74; 1KNU; 1NYX; 1PRG; 1RDT.    
FunctionReceptor 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.    
SequenceMGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL LQVIKKTETDMSLHPLLQEIYKDLY
Related US Patent6,403,656
6,462,046
6,498,174
6,646,008
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (2S)-2-[22]
(2S)-2-[22]
(2S)-2-[22]
(9S,10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid[22]
(9Z,11E,13S)-13-hydroxyoctadeca-9,11-dienoic acid[22]
2-chloro-5-nitro-N-phenylbenzamide[22]
3- (5-methoxy-1H-indol-3-yl)propanoic acid[22]
TESAGLITAZAR[23]
Agonist15-deoxy-Delta (12, 14)-prostaglandin J[5]
Ciglitazone[24]
GSK-677954[21]
GW7845[25]
Genistein[19]
Glitazone[9]
Netoglitazone[20]
Pioglitazone[16]
Rosiglitazone[16]
Rosiglitazone & metformin[18]
Rosiglitazone & simvastatin[18]
Rosiglitazone XR[18]
Thiazolidinedione[16]
Troglitazone[5][17][16]
LigandPCG1[26]
MultitargetGSK-677954[21]
Netoglitazone[20]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Gene expression profile after peroxisome proliferator activator receptor-gamma ligand administration in dextran sodium sulfate mice. J Gastroenterol. 2002 Nov;37 Suppl 14:62-6. To Reference
Ref 2Peroxisome proliferator-activated receptor-gamma: therapeutic target for diseases beyond diabetes: quo vadis? Expert Opin Investig Drugs. 2004 Mar;13(3):215-28. To Reference
Ref 3PPARgamma and atherosclerosis: effects on cell growth and movement. Arterioscler Thromb Vasc Biol. 2001 Dec;21(12):1891-5. To Reference
Ref 4Inhibition of the transcription factors AP-1 and NF-kappaB in CD4 T cells by peroxisome proliferator-activated receptor gamma ligands. Int Immunopharmacol. 2001 Apr;1(4):803-12. To Reference
Ref 5Expression 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. To Reference
Ref 6Peroxisome proliferator-activated receptor gamma agonists: potential use for treating chronic inflammatory diseases. Arthritis Rheum. 2002 Mar;46(3):598-605. To Reference
Ref 7PPARgamma and inflammatory bowel disease: a new therapeutic target for ulcerative colitis and Crohn's disease. Trends Mol Med. 2001 Aug;7(8):329-31. To Reference
Ref 8PPAR-gamma agonists: therapeutic role in diabetes, inflammation and cancer. Trends Pharmacol Sci. 2000 Dec;21(12):469-74. To Reference
Ref 9Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42. To Reference
Ref 10Peroxisome proliferator activated receptor gamma: a potential therapeutic target in the management of ischaemic heart disease. Heart. 2001 Sep;86(3):255-8. To Reference
Ref 11Peroxisome proliferator activated receptor-gamma, leptin and tumor necrosis factor-alpha mRNA expression during very low calorie diet in subcutaneous adipose tissue in obese women. Diabetes Metab Res Rev. 1999 Mar-Apr;15(2):92-8. To Reference
Ref 12Regulatory effects of peroxisome proliferator-activated receptor gamma on the growth of pancreatic carcinoma. Zhonghua Nei Ke Za Zhi. 2003 Jul;42(7):479-82. To Reference
Ref 13The effect of peroxisome proliferator-activated receptor-gamma ligand on urological cancer cells. Int J Mol Med. 2003 Dec;12(6):861-5. To Reference
Ref 14Expression of peroxisome proliferator-activated receptors in human testicular cancer and growth inhibition by its agonists. Urology. 2002 Sep;60(3):542-7. To Reference
Ref 15Mutant thyroid hormone receptor beta represses the expression and transcriptional activity of peroxisome proliferator-activated receptor gamma during thyroid carcinogenesis. Cancer Res. 2003 Sep 1;63(17):5274-80. To Reference
Ref 16Functional 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. To Reference
Ref 17Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 18GSK. Product Development Pipeline. February 2009. To Reference
Ref 19Effect of dietary genistein on Phase II and antioxidant enzymes in rat liver. Cancer Genomics Proteomics. 2009 Mar-Apr;6(2):85-92. To Reference
Ref 20Evolution of peroxisome proliferator-activated receptor agonists. Ann Pharmacother. 2007 Jun;41(6):973-83. Epub 2007 May 22. To Reference
Ref 21Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58. To Reference
Ref 22Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 23J Med Chem. 2004 Aug 12;47(17):4118-27.Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. To Reference
Ref 24New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. To Reference
Ref 25A 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. To Reference
Ref 26Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

 
   
           
 
Computer-aided Drug Design
About BIDD | Databases | Software | Teaching | Research |  Links

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543