Target Information

Target General Infomation
Target ID
T34596
Former ID
TTDR00178
Target Name
DNA gyraseA subunit
Gene Name
gyrA
Synonyms
DNA gyrasesubunit A; GyrA; gyrA
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]
Cystic fibrosis [ICD9: 277; ICD10: E84]
Otitis externa [ICD10: H60]
Function
DNA gyrasenegatively supercoils closed circular double- stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings.
BioChemical Class
ATP-hydrolyzing DNA topoisomerase
Target Validation
T34596
UniProt ID
P43700
EC Number
EC 5.99.1.3
Sequence
MTDSIQSSITPVNIEEELKSSYLDYAMSVIVGRALPDVRDGLKPVHRRVLFSMDREGNTA
NKKYVKSARVVGDVIGKYHPHGDSAVYDTIVRMAQPFSLRYMLVDGQGNFGSIDGDAPAA
MRYTEVRMQKITQALLTDLDKETVNFSPNYDGELMIPDVLPTRIPALLANGSSGIAVGMA
TNIPPHNLNEVLNGCLAYIDKNEITIDELMQHIPGPDFPTAALINGRKGIEEAYRTGRGK
VYVRARATVETNEKGREQIIVSELPYQVNKAKLVEKIAELIREKKIEGISNITDLSNKEG
IRIEIDIKRDAVGEVVLNHLYSLTQMQVTFGINMVALDHGQPRLFNLKEIIEAFVLHRRE
VVTRRSIFELRKARERTHILEGLAVARSNIDEMIAIIRNSKNREEAATSISSRSWTLHSD
IINLLDASARPDELEENLGIQGEQYYLSPAQVNAILELRLHRLTGIAFEEVIKEYEELLV
KIADLLHILSSAERLMEVIREELEEVKAQFGDDRLTEITAASGDIDLEDLIAQEDVVVTL
SHEGYVKYQPLTDYEAQRRGGKGKSATKMKEEDFIEKLLVANTHDTILCFSSRGRLYWLK
VYQLPQASRGARGRPIVNILPLQENERITAILPVSAYEEDKFVVMATAGGIVKKIALTEF
SRPRSNGIIALNLRDEDELIGVDITDGSNEIMLFSSQGRVVRFAENAVRAMGRLATGVRG
IKLALTNDISDDESAVEIEDISDDNAEASLDLNIDKVVSLVVPKGEGAILTATQNGYGKR
TQLSEYPTKSRNTKGVISIKVSERNGKVVAATQVEETDQIMLITDAGTLVRTRVSEVSIV
GRNTQGVRLIRTADDEHVVSLERVCDADEDDSLEESSSEE
Drugs and Mode of Action
Drug(s) Cetraxal Otic Drug Info Phase 3 Otitis externa [530962], [538048]
Inhaled liposomal ciprofloxacin Drug Info Phase 2 Cystic fibrosis [550263]
Inhibitor ACH-702 Drug Info [530950]
Modulator Cetraxal Otic Drug Info [530962], [538048], [544493]
Inhaled liposomal ciprofloxacin Drug Info [544493]
References
Ref 530962DNA topoisomerases and their poisoning by anticancer and antibacterial drugs. Chem Biol. 2010 May 28;17(5):421-33.
Ref 538048DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92.
Ref 550263Inhaled Ciprofloxacin for the Management of Infections in Non-Cystic Fibrosis Bronchiectasis (BE) Patients
Ref 530950Antimicrob Agents Chemother. 2010 Aug;54(8):3478-80. Epub 2010 Jun 1.In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
Ref 530962DNA topoisomerases and their poisoning by anticancer and antibacterial drugs. Chem Biol. 2010 May 28;17(5):421-33.
Ref 538048DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92.
Ref 544493Selective Targeting of Topoisomerase IV and DNA Gyrase in Staphylococcus aureus: Different Patterns of Quinolone- Induced Inhibition of DNA Synthesis. Antimicrob Agents Chemother. 2000 August; 44(8):2160-2165.

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