Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00235

Target Information
NameEnoyl-ACP reductase    
Type of targetSuccessful target    
SynonymsEnoyl-ACP reductase FabI    
Enoyl-acyl carrier protein reductase    
Enoyl-acyl carrier reductase    
Enoyl-acyl-carrier protein reductase    
FABI    
NADH-dependent enoyl-ACP reductase    
DiseaseBacterial infections
[ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104   ICD10: A00-A09, A15-A19, A20-A28, A30-A49, A65-A69, A70-A74, A75-A79]
[1][2]
Malaria
[ICD9: 084   ICD10: B50-B54]
[3][4]
Drug(s)TriclosanApprovedBacterial infections[4][3][1]
BioChemical ClassOxidoreductases acting on the CH-CH group of donors    
EC NumberEC 1.3.1.9
PathwayFatty acid biosynthesis
Metabolic pathways
UniProt IDP0AEK4
P0AEK5
P0AEK6
Q965D5
Q9BH77
PDB Structure1NHG; 1NHW; 1NNU; 1VRW; 1ZW1; 2NQ8; 2O2Y; 2OL4; 2OOS; 2OP0; 2OP1.    
SequenceMNKISQRLLFLFLHFYTTVCFIQNNTQKTFHNVLQNEQIRGKEKAFYRKEKRENIFIGNK MKHVHNMNNTHNNNHYMEKEEQDASNINKIKEENKNEDICFIAGIGDTNGYGWGIAKELS KRNVKIIFGIWPPVYNIFMKNYKNGKFDNDMIIDKDKKMNILDMLPFDASFDTANDIDEE TKNNKRYNMLQNYPIEDVANLIHQKYGKINMLVHSLANAKEVQKDLLNTSRKGYLDALSK SSYSLISLCKYFVNIMKPQSSIISLTYHASQKVVPGYGGGMSSAKAALESDTRVLAYHLG RNYNIRINTISAGPLKSRAATAINKLNNTYENNTNQNKNRNSHDVHNIMNNSGEKEEKKN SASQNYTFIDYAIEYSEKYAPLRQKLLSTDIGSVASFLLSRESRAITGQTIYVDNGLNIM FLPDDIYRNENE
Related US Patent6,372,752
6,503,903
Target ValidationClick to Find Target Validation Information.    
Inhibitor (-)-CATECHINGALLATE[5]
2- (2,4-dichlorophenoxy)-5-[6]
2- (2,4-dichlorophenoxy)-5-[7]
2- (2,4-dichlorophenoxy)-5-ethylphenol[7]
2- (2,4-dichlorophenoxy)-5-isobutylphenol[6]
2- (2,4-dichlorophenoxy)-5-isopentylphenol[6]
2- (2,4-dichlorophenoxy)-5-methylphenol[7]
2- (2,4-dichlorophenoxy)-5-phenethylphenol[6]
2- (2,4-dichlorophenoxy)-5-propylphenol[7]
2- (2-[8]
2- (2-[6]
2- (4-amino-2-chlorophenoxy)-5-chlorophenol[9]
2- (4-chloro-2-hydroxyphenoxy)benzenaminium[6]
3,7-dihydroxy-flavone[5]
3-chloro-4- (4-chloro-2-hydroxyphenoxy)benzamide[9]
4- (2,4-dichloro-phenoxy)-2'-methyl-biphenyl-3-ol[7]
4- (2,4-dichloro-phenoxy)-4'-fluoro-biphenyl-3-ol[7]
4- (2,4-dichloro-phenoxy)-biphenyl-3-ol[7]
4- (2,4-dichlorophenoxy)-3'-methylbiphenyl-3-ol[6]
4- (2,4-dichlorophenoxy)-3-hydroxybenzonitrile[7]
4- (2,4-dichlorophenoxy)-4'-methylbiphenyl-3-ol[6]
4- (2-Thienyl)-1-[10]
5-benzyl-2- (2,4-dichlorophenoxy)phenol[6]
5-butyl-2- (2,4-dichlorophenoxy)phenol[6]
5-chloro-2- (2-chloro-4-hydroxyphenoxy)phenol[9]
5-chloro-2- (2-chloro-4-nitrophenoxy)phenol[9]
BUTEIN[11]
Beta-D-Glucose[10]
Diazaborines[1]
EPICATECHIN GALLATE[11]
EPIGALLOCATECHIN[11]
EPIGALOCATECHIN GALLATE[11]
FISETIN[5]
GALLOCATECHIN GALLATE[5]
ISORHAMNETIN[5]
Indole Naphthyridinone[10]
MORIN[5]
Nicotinamide-Adenine-Dinucleotide[10]
OROIDIN[12]
TRICLOSAN[13]
Thiolactomycin[4]
BinderTriclosan[4][3][1]
WL-1001[14]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Lipid biosynthesis as a target for antibacterial agents. Prog Lipid Res. 2001 Nov;40(6):467-97. To Reference
Ref 2Validation of antibacterial mechanism of action using regulated antisense RNA expression in Staphylococcus aureus. FEMS Microbiol Lett. 2004 Feb 16;231(2):177-84. To Reference
Ref 3The apicoplast as an antimalarial drug target. Drug Resist Updat. 2001 Jun;4(3):145-51. To Reference
Ref 4Novel molecular targets for antimalarial drug development. Chem Biol Drug Des. 2008 Apr;71(4):287-97. Epub 2008 Feb 22. To Reference
Ref 5J Med Chem. 2006 Jun 1;49(11):3345-53.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. To Reference
Ref 6Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. To Reference
Ref 7J Biol Chem. 2007 Aug 31;282(35):25436-44. Epub 2007 Jun 13.X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. To Reference
Ref 8Bioorg Med Chem Lett. 2006 Apr 15;16(8):2163-9. Epub 2006 Feb 8.Synthesis and biological activity of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 2: 2'-substituted triclosan derivatives. To Reference
Ref 9Bioorg Med Chem Lett. 2005 Dec 1;15(23):5247-52. Epub 2005 Sep 29.Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4'-substituted triclosan derivatives. To Reference
Ref 10Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 11J Med Chem. 2007 Feb 22;50(4):765-75. Epub 2007 Jan 31.Green tea catechins potentiate triclosan binding to enoyl-ACP reductase from Plasmodium falciparum (PfENR). To Reference
Ref 12Bioorg Med Chem. 2007 Nov 1;15(21):6834-45. Epub 2007 Aug 22.Marine natural products from the Turkish sponge Agelas oroides that inhibit the enoyl reductases from Plasmodium falciparum, Mycobacterium tuberculosis and Escherichia coli. To Reference
Ref 13Berman 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 14Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. To Reference



 

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