Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTRVTMX)

• DTT Name: Bacterial Beta-ketoacyl-ACP synthase III (Bact fabH)
• Synonyms: KAS III; FabH; EcFabH; Condensing enzyme FabH; Beta-ketoacyl-acyl carrier protein synthase III; Acetoacetyl-acyl carrier protein synthase; Acetoacetyl-ACP synthase; 3-oxoacyl-[acyl-carrier-protein] synthase III
• Gene Name: Bact fabH
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Acyltransferase
• UniProt ID: FABH_ECOLI
• TTD ID: T72444
• EC Number: EC 2.3.1.180
• Sequence:
  MYTKIIGTGSYLPEQVRTNADLEKMVDTSDEWIVTRTGIRERHIAAPNETVSTMGFEAAT
  RAIEMAGIEKDQIGLIVVATTSATHAFPSAACQIQSMLGIKGCPAFDVAAACAGFTYALS
  VADQYVKSGAVKYALVVGSDVLARTCDPTDRGTIIIFGDGAGAAVLAASEEPGIISTHLH
  ADGSYGELLTLPNADRVNPENSIHLTMAGNEVFKVAVTELAHIVDETLAANNLDRSQLDW
  LVPHQANLRIISATAKKLGMSMDNVVVTLDRHGNTSAASVPCALDEAVRDGRIKPGQLVL
  LEAFGGGFTWGSALVRF
• 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.
• KEGG Pathway:
  Fatty acid biosynthesis (ecj00061)
  Metabolic pathways (ecj01100)
  Fatty acid metabolism (ecj01212)
• BioCyc Pathway:
  MetaCyc:FABH-MON
  EcoCyc:FABH-MON

Molecular Interaction Atlas (MIA) of This DTT

18 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-(3-Phenoxy-benzoylamino)-benzoic acid	DM6GLEA	Discovery agent	N.A.	Investigative	[2]
2-(4-Bromo-3-phenoxy-benzoylamino)-benzoic acid	DMY8GZP	Discovery agent	N.A.	Investigative	[2]
2-(4-chlorophenylsulfonyl)naphthalene-1,4-diol	DMJORCV	Discovery agent	N.A.	Investigative	[3]
2-(4-Fluoro-3-phenoxy-benzoylamino)-benzoic acid	DMGLEX5	Discovery agent	N.A.	Investigative	[2]
2-(4-propylphenylsulfonyl)naphthalene-1,4-diol	DMXC20R	Discovery agent	N.A.	Investigative	[3]
2-(methylsulfonyl)naphthalene-1,4-diol	DM1SIQD	Discovery agent	N.A.	Investigative	[3]
2-(naphthalen-2-ylsulfonyl)naphthalene-1,4-diol	DMEXBUF	Discovery agent	N.A.	Investigative	[3]
2-(p-tolylthio)naphthalene-1,4-dione	DMON1A5	Discovery agent	N.A.	Investigative	[3]
2-(phenylsulfonyl)naphthalene-1,4-diol	DMAKR2E	Discovery agent	N.A.	Investigative	[3]
2-Fluoro-6-(3-phenoxy-benzoylamino)-benzoic acid	DMP8OXL	Discovery agent	N.A.	Investigative	[2]
2-Hydroxy-6-(3-phenoxy-benzoylamino)-benzoic acid	DMB3Y8H	Discovery agent	N.A.	Investigative	[2]
2-tosylanthracene-1,4-diol	DMOFDVE	Discovery agent	N.A.	Investigative	[3]
2-tosylbenzene-1,4-diol	DM8LS6H	Discovery agent	N.A.	Investigative	[3]
2-tosylnaphthalene	DM2OUG0	Discovery agent	N.A.	Investigative	[3]
2-Tosylnaphthalene-1,4-diol	DM5FHO4	Discovery agent	N.A.	Investigative	[3]
2-tosylnaphthalene-1,4-dione	DMK9OYM	Discovery agent	N.A.	Investigative	[3]
2-[3-(Pyridin-4-yloxy)-benzoylamino]-benzoic acid	DM5ETL9	Discovery agent	N.A.	Investigative	[2]
Thiolactomycin	DMBAWDG	Malaria	1F40-1F45	Investigative	[1]

References

• [1] The apicoplast as an antimalarial drug target. Drug Resist Updat. 2001 Jun;4(3):145-51.
• [2] Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial age... J Med Chem. 2005 Mar 10;48(5):1596-609.
• [3] Synthesis and biological evaluation of novel sulfonyl-naphthalene-1,4-diols as FabH inhibitors. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6402-5.