Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00124

Target Information
NameCholesteryl ester transfer protein    
Type of targetClinical trial target    
SynonymsCETP    
Cholesterol ester transfer protein    
Lipid transfer protein I    
DiseaseAtherosclerosis
[ICD9: 414.0, 440   ICD10: I70]
[1]
Coronary atherosclerosis
[ICD9: 414.0, 440   ICD10: I70]
[2]
Hypercholesterolemia
[ICD9: 272.0   ICD10: E78.0]
[3]
Hyperlipidemia
[ICD9: 272.0-272.4   ICD10: E78]
[4][5][6]
Peripheral Vascular Disease
[ICD9: 443.9   ICD10: I73.9]
[4][5][6]
Drug(s)AnacetrapibPhase IIIAtherosclerosis[7][8][6][9][10]
DalcetrapibPhase IIIDyslipidemia[11]
AnacetrapibPhase IIHyperlipidemia[7][8][6]
DS-1442Phase IDyslipidemia
CP-800569DiscontinuedAtherosclerosis[12][13]
PF-3185043DiscontinuedAtherosclerosis[12][13]
R7232Suspended in Phase IDyslipidemia[11][14]
TorcetrapibTerminated in Phase IIIPeripheral Vascular Disease, Hyperlipidemia[4][5][6]
UniProt IDP11597
PDB Structure2OBD; 4EWS; 4F2A.    
FunctionInvolved in the transfer of insoluble cholesteryl esters in the reverse transport of cholesterol.    
SequenceMLAATVLTLALLGNAHACSKGTSHEAGIVCRITKPALLVLNHETAKVIQTAFQRASYPDI TGEKAMMLLGQVKYGLHNIQISHLSIASSQVELVEAKSIDVSIQNVSVVFKGTLKYGYTT AWWLGIDQSIDFEIDSAIDLQINTQLTCDSGRVRTDAPDCYLSFHKLLLHLQGEREPGWI KQLFTNFISFTLKLVLKGQICKEINVISNIMADFVQTRAASILSDGDIGVDISLTGDPVI TASYLESHHKGHFIYKNVSEDLPLPTFSPTLLGDSRMLYFWFSERVFHSLAKVAFQDGRL MLSLMGDEFKAVLETWGFNTNQEIFQEVVGGFPSQAQVTVHCLKMPKISCQNKGVVVNSS VMVKFLFPRPDQQHSVAYTFEEDIVTTVQASYSKKKLFLSLLDFQITPKTVSNLTESSSE SVQSFLQSMITAVGIPEVMSRLEVVFTALMNSKGVSLFDIINPEIITRDGFLLLQMDFGF PEHLLVDFLQSLS
Related US Patent6,387,929
6,562,976
6,573,383
6,600,045
6,706,881
Target ValidationClick to Find Target Validation Information.    
InhibitorAnacetrapib[7][8][6][9][10]
Anacetrapib[7][8][6]
CP-800569[12][13]
Dalcetrapib[11]
NSC-40331[15]
NSC-89508[15]
PF-3185043[12][13]
R7232[11][14]
SC-795[15]
TETRAHYDROQUINOLINE A[16]
TETRAHYDROQUINOLINE B[16]
Torcetrapib[4][5][6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Insulin does not regulate the promoter of cholesteryl ester transfer protein (CETP) in HIRc/pCETP-CAT cells. Mol Cell Biochem. 2000 Aug;211(1-2):1-7. To Reference
Ref 2Cholesteryl ester transfer protein: gathering momentum as a genetic marker and as drug target. Curr Opin Lipidol. 2003 Apr;14(2):173-9. To Reference
Ref 3Cholesteryl ester transfer protein and atherosclerosis. Curr Opin Lipidol. 2000 Aug;11(4):389-96. To Reference
Ref 4Safety and tolerability of dalcetrapib. Am J Cardiol. 2009 Jul 1;104(1):82-91. To Reference
Ref 5A Translational Medicine perspective of the development of torcetrapib: Does the failure of torcetrapib development cast a shadow on future development of lipid modifying agents, HDL elevation strategies or CETP as a viable molecular target for atherosclerosis? A case study of the use of biomarkers and Translational Medicine in atherosclerosis drug discovery and development. Biochem Pharmacol. 2009 Aug 15;78(4):315-25. Epub 2009 Mar 24. To Reference
Ref 6The end of the road for CETP inhibitors after torcetrapib? Curr Opin Cardiol. 2009 Jul;24(4):364-71. To Reference
Ref 7Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects. Br J Clin Pharmacol. 2009 May;67(5):520-6. Epub 2009 Feb 4. To Reference
Ref 8Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Apr;31(3):183-227. To Reference
Ref 9Merck. Product Development Pipeline. July 15 2009. To Reference
Ref 10Merck. Report of Merck. 2007. To Reference
Ref 11Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 12Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 13Pfizer. News for Pfizer. October 1 2008. To Reference
Ref 14Roche. Report of Roche. 2009. To Reference
Ref 15Eur J Med Chem. 2010 Apr;45(4):1598-617. Epub 2010 Jan 14.Discovery of new cholesteryl ester transfer protein inhibitors via ligand-based pharmacophore modeling and QSAR analysis followed by synthetic exploration. To Reference
Ref 16Bioorg Med Chem Lett. 2009 May 1;19(9):2456-60. Epub 2009 Mar 18.Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform. To Reference



 

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