Resistance mutation info of drug

Drug General Information
Drug ID D00HYK
Drug Name AFN-1252 Drug Info
Synonyms API-1252; API-1401; Antibacterial therapeutics, Affinium; Antibacterials, Affinium; Bacterial fatty acid biosynthesis inhibitors, Affinium; Galapagos program, Affinium; Antibacterial therapeutics, Affinium/GSK; Antibacterials, Affinium/GSK; FabI inhibitors (antibacterial), Affinium; AFN-1252 (oral, bacterial infection); AFN-1252 (oral, bacterial infection), Affinium
Drug Type Small molecular drug
Company Affinium pharmaceuticals
Structure D00HYK
Drug Resistance Mutations
Target Name Bacterial Staphylococcus aureus Enoyl ACP reductase (fabI) Target Info
Gene Name fabI
Uniprot ID FABI_STAA8
Species Staphylococcus aureus
Reference Sequence MLNLENKTYVIMGIANKRSIAFGVAKVLDQLGAKLVFTYRKERSRKELEKLLEQLNQPEA
HLYQIDVQSDEEVINGFEQIGKDVGNIDGVYHSIAFANMEDLRGRFSETSREGFLLAQDI
SSYSLTIVAHEAKKLMPEGGSIVATTYLGGEFAVQNYNVMGVAKASLEANVKYLALDLGP
DNIRVNAISASPIRTLSAKGVGGFNTILKEIEERAPLKRNVDQVEVGKTAAYLLSDLSSG
VTGENIHVDSGFHAIK [Staphylococcus aureus]
Targeted Disease Staphylococcus aureus infection
Drug Resistance Mutations
Mutation info Missense: M99T [555978]
Mutation info Missense: Y147H [555978]
References
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 555978Resistance to AFN-1252 arises from missense mutations in Staphylococcus aureus enoyl-acyl carrier protein reductase (FabI). J Biol Chem. 2013 Dec 20;288(51):36261-71. doi: 10.1074/jbc.M113.512905. Epub 2013 Nov 4.

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