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DNA Gyrase

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Definition: A bacterial DNA topoisomerase II that catalyzes ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. Gyrase binds to DNA as a heterotetramer consisting two A and two B subunits. In the presence of ATP, gyrase is able to convert relaxed circular DNA duplex into a superhelix. In the absence of ATP, supercoiled DNA is relaxed by DNA gyrase.      Other names gyrB Gene Product; gyrA Gene product; DNA-Gyrase; gyrB Protein; gyrA Protein; DNA Gyrase B Subunit; DNA Gyrase A Subunit
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
4-benzoyl-1-(4-methyl-imidazol-5-yl)carbonylthiosemicarbazide  0   *Imidazoles *Semicarbazides DNA Gyrase/antagonists & inhibitors. J Mol Model. 2011 Sep;17(9):2297-303.
2-(3',4'-dihydroxyphenyl)-5,7-dihydroxy-3-(2'',6''-di-O-(3'''-(4-fluorophenylpropanoyl)))galactosyl-4H-chromen-4-one  0   *Galactosides Quercetin/*analogs & derivatives DNA Gyrase/antagonists & inhibitors DNA Topoisomerase IV/antagonists & inhibitors. J Med Chem 2011 Jun 9;54(11):3686-703
novobiocin 401  0   Novobiocin/*analogs & derivatives DNA Gyrase/antagonists & inhibitors. Chem Biol 2011 Mar 25;18(3):304-13
ACH 702  0   *Thiazoles *Quinolones DNA Gyrase/antagonists & inhibitors. Antimicrob Agents Chemother 2010 May;54(5):2191-3
PF 03376056  0   *Azetidines *Indazoles DNA Gyrase/antagonists & inhibitors. Drug Metab Lett 2009 Jan;3(1):28-34
PNU-286607  0   *Heterocyclic Compounds with 4 or More Rings *Spiro Compounds DNA Gyrase/antagonists & inhibitors. J Am Chem Soc 2009 Mar 25;131(11):3991-7
7-(3-(1-aminoethyl)pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-8-methyl-1H-quinazoline-2,4-dione  0   *Pyrrolidines *Quinazolinones DNA Gyrase/antagonists & inhibitors DNA Topoisomerase IV/antagonists & inhibitors. Antimicrob Agents Chemother 2007 Apr;51(4):1191-201
3-amino-7-(3-(1-aminoethyl)pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-8-methyl-1H-quinazoline-2,4-dione  0   *Pyrrolidines *Quinazolinones DNA Gyrase/antagonists & inhibitors DNA Topoisomerase IV/antagonists & inhibitors. Antimicrob Agents Chemother 2007 Apr;51(4):1191-201
WCK 1734  0   *Quinolones DNA Gyrase/antagonists & inhibitors. Antimicrob Agents Chemother 2005 May;49(5):1949-56
5-(2-(5-chloroindol-3-yl)vinyl)pyrazole  0   *Indoles *Pyrazoles DNA Gyrase/antagonists & inhibitors. J Med Chem 2004 Jul 1;47(14):3693-6
1,3,4,5,6,7,8,9,10,12-decahydro-16-hydroxy-14-methoxy-13-methyl-4-(3-methyl-1,2,4-oxadiazol-5-yl)-6-thioxo-11,2,5-benzoxathiaazacyclotetradecine-12-one  0   *Lactams *Oxadiazoles DNA Gyrase/antagonists & inhibitors. J Med Chem 2004 Mar 11;47(6):1487-513
1,3,4,5,6,7,8,10-octahydro-14-hydroxy-12-methoxy-11-methyl-4-(3-methyl-1,2,4-oxadiazol-5-yl)-6-thioxo-9,2,5-benzoxanthiaazacyclododecine-10-one  0   *Lactams *Oxadiazoles DNA Gyrase/antagonists & inhibitors. J Med Chem 2004 Mar 11;47(6):1487-513
cinodine  52932-64-6   *Aminoglycosides *Spermidine DNA Gyrase. Antimicrob Agents Chemother 1981;20(4):425
coumermycin  4434-05-3   *Aminocoumarins DNA Gyrase/antagonists & inhibitors. Biochemistry 15(17):3769-78;1976; J Mol Biol 120:145;1978; J Mol Biol 1979;131(3):637; MGG 1979;176(1):25; MGG 1979;176(2):171; MGG 1979;177(1):169; MGG 1980;177(2):301; Mol Biol (Mosk) 1979;13(6):1341; Proc Nat Acad Sci USA 73(12):4474;1976; Proc Nat Acad Sci USA 75(10):4838;1978; Proc Nat Acad Sci USA 75(9):4125;1978

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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012
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