Therapeutic Targets Database
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TTD Target ID: TTDC00069

Target Information
NamePeroxisome proliferator activated receptor delta    
Type of targetClinical trial target    
SynonymsNUC1    
NUCI    
Nuclear hormone receptor 1    
PPAR-beta    
PPAR-delta    
PPARdelta    
Peroxisome proliferator activated receptor beta/delta    
Peroxisome proliferator-activated receptor beta    
DiseaseAtherosclerosis
[ICD9: 414.0, 440   ICD10: I70]
[1]
Hyperlipidemia
[ICD9: 272.0-272.4   ICD10: E78]
[2]
Inflammation[1]
Metabolic Disease
[ICD9: 270-279   ICD10: E70-E89]
[2]
Metabolic syndrome X
[ICD9: 277.7   ICD10: E88.81]
[3]
Noninsulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[4]
Obesity
[ICD9: 278   ICD10: E66]
[5][4]
Skin diseases[3]
Drug(s)MBX-8025Phase II completedHyperlipidemia, Obesity[6]
NetoglitazonePhase IINon-alcoholic fatty liver disease (NAFLD)[7]
KD3010Phase IMetabolic Disease, Obesity[8]
GSK-677954Discontinued in Phase IINon-alcoholic fatty liver disease (NAFLD)[9]
KD-3020PreclinicalNon-alcoholic fatty liver disease (NAFLD)[9]
BioChemical ClassZinc-finger    
PathwayAcute myeloid leukemia
PPAR signaling pathway
Pathways in cancer
Wnt signaling pathway
UniProt IDQ03181
PDB Structure1GWX; 1Y0S; 2AWH; 2B50; 2BAW; 2ENV; 2GWX; 2J14; 2Q5G; 2XYJ; 2XYW; 2XYX; 2ZNP; 2ZNQ; 3D5F; 3DY6; 3ET2; 3GWX; 3GZ9; 3OZ0; 3PEQ; 3SP9; 3TKM.    
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.    
SequenceMEQPQEEAPEVREEEEKEEVAEAEGAPELNGGPQHALPSSSYTDLSRSSSPPSLLDQLQM GCDGASCGSLNMECRVCGDKASGFHYGVHACEGCKGFFRRTIRMKLEYEKCERSCKIQKK NRNKCQYCRFQKCLALGMSHNAIRFGRMPEAEKRKLVAGLTANEGSQYNPQVADLKAFSK HIYNAYLKNFNMTKKKARSILTGKASHTAPFVIHDIETLWQAEKGLVWKQLVNGLPPYKE ISVHVFYRCQCTTVETVRELTEFAKSIPSFSSLFLNDQVTLLKYGVHEAIFAMLASIVNK DGLLVANGSGFVTREFLRSLRKPFSDIIEPKFEFAVKFNALELDDSDLALFIAAIILCGD RPGLMNVPRVEAIQDTILRALEFHLQANHPDAQYLFPKLLQKMADLRQLVTEHAQMMQRI KKTETETSLHPLLQEIYKDMY
Related US Patent6,723,740
6,787,552
Target ValidationClick to Find Target Validation Information.    
Inhibitor (11E)-OCTADEC-11-ENOIC ACID[10]
GSK-0660[11]
GSK-3787[11]
GW-501516[11]
Heptyl-Beta-D-Glucopyranoside[10]
L-165461[12]
L-796449[12]
AgonistGSK-677954[9]
KD-3020[9]
KD3010[8]
MBX-8025[6]
Netoglitazone[7]
MultitargetGSK-677954[9]
Netoglitazone[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Transcriptional repression of atherogenic inflammation: modulation by PPARdelta. Science. 2003 Oct 17;302(5644):453-7. Epub 2003 Sep 11. To Reference
Ref 2CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 3Peroxisome proliferator-activated receptors beta/delta: emerging roles for a previously neglected third family member. Curr Opin Lipidol. 2003 Apr;14(2):129-35. To Reference
Ref 4Genetic polymorphisms in peroxisome proliferator-activated receptor delta associated with obesity. Diabetes. 2004 Mar;53(3):847-51. To Reference
Ref 5Peroxisome-proliferator-activated receptor delta activates fat metabolism to prevent obesity. Cell. 2003 Apr 18;113(2):159-70. To Reference
Ref 6Safety and Benefit of MBX-8025 With and Without Commonly Used Statins in Moderately Overweight Patients With High Cholesterol. U. S. National Institute of Health. 2008 To Reference
Ref 7Evolution of peroxisome proliferator-activated receptor agonists. Ann Pharmacother. 2007 Jun;41(6):973-83. Epub 2007 May 22. To Reference
Ref 8Kalypsys nearing completion of phase Ia study of KD3010 for metabolic disorders. Kalypsys. 2007 To Reference
Ref 9Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58. To Reference
Ref 10Nucleic Acids Res. 2011 January; 39(Database issue): D1035¨CD1041. DrugBank 3.0: a comprehensive resource for ¡®Omics¡¯ research on drugs To Reference
Ref 11J Med Chem. 2010 Feb 25;53(4):1857-61.Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist. To Reference
Ref 12Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.Phenylacetic acid derivatives as hPPAR agonists. To Reference



 

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