Target Information

Target General Infomation
Target ID
T72444
Former ID
TTDR00361
Target Name
Beta-ketoacyl-ACP synthase III
Gene Name
fabH
Synonyms
3-oxoacyl-[acyl-carrier-protein] synthase III; Acetoacetyl-ACP synthase; Acetoacetyl-acyl carrier protein synthase; Beta-ketoacyl-acyl carrier protein synthase III; Condensing enzyme FabH; EcFabH; FabH; KAS III; fabH
Target Type
Research
Disease Malaria [ICD10: B54]
Function
Catalyzes the condensation reaction of fatty acid synthesis by the addition to an acyl acceptor of two carbons from malonyl-ACP. Catalyzes the first condensation reaction which initiates fatty acid synthesis and may therefore play a role in governing the total rate of fatty acid production. Possesses both acetoacetyl-ACP synthase and acetyl transacylase activities. Has some substrate specificity for acetyl-CoA. Its substrate specificity determines the biosynthesis of straight-chain of fatty acids instead of branched-chain.
BioChemical Class
Acyltransferase
Target Validation
T72444
UniProt ID
P0A6R0
EC Number
EC 2.3.1.41
Sequence
MYTKIIGTGSYLPEQVRTNADLEKMVDTSDEWIVTRTGIRERHIAAPNETVSTMGFEAAT
RAIEMAGIEKDQIGLIVVATTSATHAFPSAACQIQSMLGIKGCPAFDVAAACAGFTYALS
VADQYVKSGAVKYALVVGSDVLARTCDPTDRGTIIIFGDGAGAAVLAASEEPGIISTHLH
ADGSYGELLTLPNADRVNPENSIHLTMAGNEVFKVAVTELAHIVDETLAANNLDRSQLDW
LVPHQANLRIISATAKKLGMSMDNVVVTLDRHGNTSAASVPCALDEAVRDGRIKPGQLVL
LEAFGGGFTWGSALVRF
Inhibitor 2-(3-Phenoxy-benzoylamino)-benzoic acid Drug Info [527457]
2-(4-Bromo-3-phenoxy-benzoylamino)-benzoic acid Drug Info [527457]
2-(4-chlorophenylsulfonyl)naphthalene-1,4-diol Drug Info [529797]
2-(4-Fluoro-3-phenoxy-benzoylamino)-benzoic acid Drug Info [527457]
2-(4-propylphenylsulfonyl)naphthalene-1,4-diol Drug Info [529797]
2-(methylsulfonyl)naphthalene-1,4-diol Drug Info [529797]
2-(naphthalen-2-ylsulfonyl)naphthalene-1,4-diol Drug Info [529797]
2-(p-tolylthio)naphthalene-1,4-dione Drug Info [529797]
2-(phenylsulfonyl)naphthalene-1,4-diol Drug Info [529797]
2-Fluoro-6-(3-phenoxy-benzoylamino)-benzoic acid Drug Info [527457]
2-Hydroxy-6-(3-phenoxy-benzoylamino)-benzoic acid Drug Info [527457]
2-tosylanthracene-1,4-diol Drug Info [529797]
2-tosylbenzene-1,4-diol Drug Info [529797]
2-tosylnaphthalene Drug Info [529797]
2-Tosylnaphthalene-1,4-diol Drug Info [529797]
2-tosylnaphthalene-1,4-dione Drug Info [529797]
2-[3-(Pyridin-4-yloxy)-benzoylamino]-benzoic acid Drug Info [527457]
Binder Thiolactomycin Drug Info [535329]
References
Ref 527457J Med Chem. 2005 Mar 10;48(5):1596-609.Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents.
Ref 529797Bioorg Med Chem Lett. 2008 Dec 15;18(24):6402-5. Epub 2008 Oct 25.Synthesis and biological evaluation of novel sulfonyl-naphthalene-1,4-diols as FabH inhibitors.
Ref 535329The apicoplast as an antimalarial drug target. Drug Resist Updat. 2001 Jun;4(3):145-51.

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