Target Information

Target General Infomation
Target ID
T23036
Former ID
TTDI02067
Target Name
Staphylococcus aureus Enoyl ACP reductase
Gene Name
fabI
Synonyms
ENR; Enoyl[acylcarrierprotein] reductase [NADPH] FabI; NADPHdependent enoylACP reductase; fabI
Target Type
Clinical Trial
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Methicillin-resistant staphylococcus aureus infection [ICD10: B95.62]
Staphylococcus aureus infection [ICD10: B95.6]
Function
Catalyzes the reduction of a carbon-carbon double bond in an enoyl moiety that is covalently linked to an acyl carrier protein (ACP). It has a preference for a long chain (C12) substrate compared to the shorter (C4) acyl group. Involved in the elongation cycle of fatty acid which are used in the lipid metabolism (By similarity).
BioChemical Class
Short-chain dehydrogenases reductases
UniProt ID
Q2FZQ3
EC Number
EC=1.3.1.10
Sequence
MLNLENKTYVIMGIANKRSIAFGVAKVLDQLGAKLVFTYRKERSRKELEKLLEQLNQPEA
HLYQIDVQSDEEVINGFEQIGKDVGNIDGVYHSIAFANMEDLRGRFSETSREGFLLAQDI
SSYSLTIVAHEAKKLMPEGGSIVATTYLGGEFAVQNYNVMGVAKASLEANVKYLALDLGP
DNIRVNAISASPIRTLSAKGVGGFNTILKEIEERAPLKRNVDQVEVGKTAAYLLSDLSSG
VTGENIHVDSGFHAIK
Drugs and Mode of Action
Drug(s) AFN-1252 Drug Info Phase 2 Staphylococcus aureus infection [532242]
CG-400549 Drug Info Phase 2 Bacterial infections [523897]
MUT-056399 Drug Info Preclinical Methicillin-resistant staphylococcus aureus infection [548048]
Inhibitor AFN-1252 Drug Info [532242]
CG-400549 Drug Info [528783]
Modulator MUT-056399 Drug Info [531594]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
DRM DRM Info
Pathways
KEGG Pathway Fatty acid biosynthesis
Biotin metabolism
Metabolic pathways
Fatty acid metabolism
References
Ref 523897ClinicalTrials.gov (NCT01593761) Phase 2a Study of CG400549 for the Treatment of cABSSSI Caused by Methicillin-resistant Staphylococcus Aureus. U.S. National Institutes of Health.
Ref 532242Activity of AFN-1252, a novel FabI inhibitor, against Staphylococcus aureus in an in vitro pharmacodynamic model simulating human pharmacokinetics. J Chemother. 2013 Feb;25(1):32-5.
Ref 548048Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021501)
Ref 528783In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea. Antimicrob Agents Chemother. 2007 Jul;51(7):2591-3. Epub 2007 Apr 9.
Ref 531594The MUT056399 inhibitor of FabI is a new antistaphylococcal compound. Antimicrob Agents Chemother. 2011 Oct;55(10):4692-7.
Ref 532242Activity of AFN-1252, a novel FabI inhibitor, against Staphylococcus aureus in an in vitro pharmacodynamic model simulating human pharmacokinetics. J Chemother. 2013 Feb;25(1):32-5.

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