Target Information

Target General Infomation
Target ID
T53748
Former ID
TTDS00235
Target Name
Enoyl-ACP reductase
Gene Name
fabI
Synonyms
Enoyl-ACP reductase FabI; Enoyl-acyl carrier protein reductase; Enoyl-acyl carrier reductase; Enoyl-acyl-carrier protein reductase; FABI; NADH-dependent enoyl-ACP reductase; fabI
Target Type
Successful
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Infection of P. falciparum; Trypanosoma [ICD9: 084, 086; ICD10: B50-B54, B56]
Malaria [ICD10: B54]
Function
Catalyzes the reduction of a carbon-carbon double bond in an enoyl moiety that is covalently linked to an acyl carrier protein (ACP). Involved in the elongation cycle of fatty acid which are used in the lipid metabolism and in the biotin biosynthesis (By similarity).
BioChemical Class
Oxidoreductases acting on CH-CH group of donors
Target Validation
T53748
UniProt ID
Q965D5
EC Number
EC 1.3.1.9
Sequence
MNKISQRLLFLFLHFYTTVCFIQNNTQKTFHNVLQNEQIRGKEKAFYRKEKRENIFIGNK
MKHVHNMNNTHNNNHYMEKEEQDASNINKIKEENKNEDICFIAGIGDTNGYGWGIAKELS
KRNVKIIFGIWPPVYNIFMKNYKNGKFDNDMIIDKDKKMNILDMLPFDASFDTANDIDEE
TKNNKRYNMLQNYPIEDVANLIHQKYGKINMLVHSLANAKEVQKDLLNTSRKGYLDALSK
SSYSLISLCKYFVNIMKPQSSIISLTYHASQKVVPGYGGGMSSAKAALESDTRVLAYHLG
RNYNIRINTISAGPLKSRAATAINKLNNTYENNTNQNKNRNSHDVHNIMNNSGEKEEKKN
SASQNYTFIDYAIEYSEKYAPLRQKLLSTDIGSVASFLLSRESRAITGQTIYVDNGLNIM
FLPDDIYRNENE
Drugs and Mode of Action
Drug(s) Triclosan Drug Info Approved Bacterial infections [536463]
Inhibitor (-)-CATECHINGALLATE Drug Info [528213]
2-(2,4-dichlorophenoxy)-5-(2-methylbutyl)phenol Drug Info [529962]
2-(2,4-dichlorophenoxy)-5-(3-phenylpropyl)phenol Drug Info [528892]
2-(2,4-dichlorophenoxy)-5-ethylphenol Drug Info [528892]
2-(2,4-dichlorophenoxy)-5-isobutylphenol Drug Info [529962]
2-(2,4-dichlorophenoxy)-5-isopentylphenol Drug Info [529962]
2-(2,4-dichlorophenoxy)-5-methylphenol Drug Info [528892]
2-(2,4-dichlorophenoxy)-5-phenethylphenol Drug Info [529962]
2-(2,4-dichlorophenoxy)-5-propylphenol Drug Info [528892]
2-(2-((benzylamino)methyl)phenoxy)-5-chlorophenol Drug Info [528023]
2-(4-amino-2-chlorophenoxy)-5-chlorophenol Drug Info [527778]
2-(4-chloro-2-hydroxyphenoxy)benzenaminium Drug Info [529962]
3,7-dihydroxy-flavone Drug Info [528213]
3-chloro-4-(4-chloro-2-hydroxyphenoxy)benzamide Drug Info [527778]
4-(2,4-dichloro-phenoxy)-2'-methyl-biphenyl-3-ol Drug Info [528892]
4-(2,4-dichloro-phenoxy)-4'-fluoro-biphenyl-3-ol Drug Info [528892]
4-(2,4-dichloro-phenoxy)-biphenyl-3-ol Drug Info [528892]
4-(2,4-dichlorophenoxy)-3'-methylbiphenyl-3-ol Drug Info [529962]
4-(2,4-dichlorophenoxy)-3-hydroxybenzonitrile Drug Info [528892]
4-(2,4-dichlorophenoxy)-4'-methylbiphenyl-3-ol Drug Info [529962]
4-(2-Thienyl)-1-(4-Methylbenzyl)-1h-Imidazole Drug Info [551393]
5-benzyl-2-(2,4-dichlorophenoxy)phenol Drug Info [529962]
5-butyl-2-(2,4-dichlorophenoxy)phenol Drug Info [529962]
5-chloro-2-(2-chloro-4-hydroxyphenoxy)phenol Drug Info [527778]
5-chloro-2-(2-chloro-4-nitrophenoxy)phenol Drug Info [527778]
Beta-D-Glucose Drug Info [551393]
BUTEIN Drug Info [528645]
Diazaborines Drug Info [535276]
EPIGALOCATECHIN GALLATE Drug Info [528645]
FISETIN Drug Info [528213]
GALLOCATECHIN GALLATE Drug Info [528213]
Indole Naphthyridinone Drug Info [551393]
ISORHAMNETIN Drug Info [528213]
MORIN Drug Info [528213]
Nicotinamide-Adenine-Dinucleotide Drug Info [551393]
OROIDIN Drug Info [529012]
Thiolactomycin Drug Info [536636]
Binder Triclosan Drug Info [535276], [535329], [536636]
WL-1001 Drug Info [536135]
References
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 527778Bioorg 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.
Ref 528023Bioorg 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.
Ref 528213J 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.
Ref 528645J 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).
Ref 528892J 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.
Ref 529012Bioorg 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.
Ref 529962Eur 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.
Ref 535276Lipid biosynthesis as a target for antibacterial agents. Prog Lipid Res. 2001 Nov;40(6):467-97.
Ref 535329The apicoplast as an antimalarial drug target. Drug Resist Updat. 2001 Jun;4(3):145-51.
Ref 536135Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
Ref 536636Novel molecular targets for antimalarial drug development. Chem Biol Drug Des. 2008 Apr;71(4):287-97. Epub 2008 Feb 22.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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