ライフサイエンスコーパス: gyrase

1 genes potentially encode subunits of a plant gyrase.

2 ant enzymes than moxifloxacin did against WT gyrase.

3 the detailed mechanism of SD8 inhibition of gyrase.

4 y Streptomyces antibioticus that targets DNA gyrase.

5 ut until now were shown for no other reverse gyrase.

6 a bacterial topoisomerase, Escherichia coli gyrase.

7 biotics which target the GyrA subunit of DNA gyrase.

8 kage by Streptococcus pneumoniae topo IV and gyrase.

9 been reported for Mycobacterium tuberculosis gyrase.

10 site in the GyrA subunit of M. tuberculosis gyrase.

11 ling and DNA-stimulated ATPase activities of gyrase.

12 m of positive supercoil induction by reverse gyrase.

13 iocin, which targets the GyrB subunit of DNA gyrase.

14 consistent with allosteric inhibition of DNA gyrase.

15 e beta-pinwheel and is a hallmark feature of gyrases.

16 atalyzed by M. tuberculosis gyrase and other gyrases.

17 ymes that includes RNA polymerase (RNAP)(6), gyrase(2), a viral DNA packaging motor(7) and DNA recomb

18 e interaction where loop1 interacts with the gyrase A 'tower' and loop2 with the gyrase B TOPRIM doma

19 ovember 2015, UCLA Health introduced a rapid gyrase A (gyrA) genotypic assay for prediction of Neisse

20 enicol resistance, penicillin resistance, or gyrase A function can effectively be reduced in their ex

21 the isolates were screened for integrons and gyrase A gene mutations.

22 plexed with the N-terminal domain of the DNA gyrase A protein (GyrA) suggested that four SD8 molecule

23 al aminocoumarin that inhibits bacterial DNA gyrase, a member of the GHKL proteins superfamily.

24 Gyrase, a prokaryotic heterotetrameric type IIA topo, in

25 Gyrase, a prokaryotic type IIA topoisomerase, consumes A

26 determined the structure of Escherichia coli gyrase, a type IIA topoisomerase bound to YacG, a recent

27 sistance to other antibiotics, including the gyrase-acting fluoroquinolones.

28 pe is not the sole regulatory determinant of gyrase activity and instead indicate that an inability t

29 se and suggest a model for the modulation of gyrase activity by Ca(2+) binding.

30 t CTD functions can be fine-tuned to control gyrase activity in a highly sophisticated manner.

31 ical network) resulting in inhibition of DNA gyrase activity, the primary target of fluoroquinolones.

32 ridones that kills Mtb by inhibiting the DNA gyrase activity.

33 rate negative regulator of Bacillus subtilis gyrase activity.

34 dependent homeostatic mechanisms such as DNA-gyrase activity.

35 Understanding the molecular details of gyrase adaptations to the specific physiological require

36 e parDE TA locus, which is thought to target gyrase although its mechanism of action is uncharacteriz

37 than moxifloxacin against WT M. tuberculosis gyrase and displayed higher activity against the mutant

38 fulfil the functions normally carried out by gyrase and DNA topoisomerase IV in other bacteria.

39 nt in complex with Staphylococcus aureus DNA gyrase and DNA, showing a new mode of inhibition that ci

40 f fluoroquinolones and related drugs with WT gyrase and enzymes carrying mutations at GyrA(A90) and G

41 basis of drug action against M. tuberculosis gyrase and how mutations in the enzyme cause resistance.

42 t show significant inhibition of E. coli DNA gyrase and hTop 1 even up to 100 muM.

43 Escherichia coli gyrase and human topoisomerase IIalpha were challenged w

44 oiling reaction catalyzed by M. tuberculosis gyrase and other gyrases.

45 ustration of mechanical interactions between gyrase and other molecular machines at the heart of chro

46 te but bind to different target enzymes (DNA gyrase and penicillin-binding proteins, respectively) an

47 hich exceeds the activity of M. tuberculosis gyrase and reaches the activity of the B. subtilis gyras

48 2+) has a regulatory role in M. tuberculosis gyrase and suggest a model for the modulation of gyrase

49 toxin CcdB prevents CcdB from inhibiting DNA gyrase and thereby averts cell death.

50 fluoroquinolones trap a cleavage complex of gyrase and topoisomerase (topo) IV inducing site-specifi

51 Measurements with Gyrase and Topoisomerase I inhibitors suggest hindrance

52 In bacteria, DNA gyrase and topoisomerase IV act ahead of the fork to kee

53 xemplified by 34, that inhibit bacterial DNA gyrase and topoisomerase IV and display potent activity

54 interacts with all the subunits of both DNA gyrase and topoisomerase IV and has measurable effects o

55 E ATP-binding sites located on bacterial DNA gyrase and topoisomerase IV and not utilized by marketed

56 Bacterial DNA gyrase and topoisomerase IV are essential enzymes that c

57 Neisseria gonorrhoeae type II topoisomerases gyrase and topoisomerase IV by AZD0914 (AZD0914 will be

58 DNA gyrase and topoisomerase IV control bacterial DNA topolo

59 Bacterial DNA gyrase and topoisomerase IV control the topological stat

60 oved inhibition of Staphylococcus aureus DNA gyrase and topoisomerase IV from both bacteria.

61 nd 27 was the most balanced inhibitor of DNA gyrase and topoisomerase IV from both E. coli and S. aur

62 Inhibition of the topoisomerases DNA gyrase and topoisomerase IV from both Gram-positive and

63 Although bacterial gyrase and topoisomerase IV have critical interactions w

64 dropyran-based molecules that are potent DNA gyrase and topoisomerase IV inhibitors and display excel

65 Research into DNA gyrase and topoisomerase IV inhibitors has become a part

66 class of compounds toward balanced dual DNA gyrase and topoisomerase IV inhibitors with antibacteria

67 structure-based optimization toward dual DNA gyrase and topoisomerase IV inhibitors with antibacteria

68 t a new antibacterial class of bacterial DNA gyrase and topoisomerase IV inhibitors.

69 egy for investigating the well-validated DNA gyrase and topoisomerase IV targets while preventing cro

70 s of Bacillus anthracis and Escherichia coli gyrase and topoisomerase IV to relax and cleave positive

71 aphylococcus aureus and Escherichia coli DNA gyrase and topoisomerase IV was identified.

72 ors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) are of interest for the dev

73 ors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) display potent activity aga

74 ors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) display potent antibacteria

75 ors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) have the potential to becom

76 a new class of bacterial topoisomerase (DNA gyrase and topoisomerase IV) inhibitors binding in the A

77 s 6 and 21 are potent inhibitors of both DNA gyrase and topoisomerase IV, displaying antibacterial ac

78 against the ATP binding pockets of both DNA gyrase and topoisomerase IV.

79 ivity of the DNA helicase might overcome DNA gyrase and topoisomerase IV.

80 nzyme-DNA cleaved complex for N. gonorrhoeae gyrase and topoisomerase IV.

81 ity through dual inhibition of bacterial DNA gyrase and topoisomerase IV.

82 itors that bind to the catalytic site of DNA gyrase and topoisomerase IV.

83 omerase IIbeta (TOP2B), and two in bacteria, gyrase and topoisomerase IV.

84 In contrast, loss of gyrase and TtAgo activity slows growth and produces long

85 ontrol element recently uncovered in E. coli gyrase and turns over ATP at a much slower rate.

86 levels of stable cleavage complexes with WT gyrase and two common resistant enzymes, GyrA(A90V) and

87 phase, whereas during exponential growth DNA gyrase and/or transcription equalizes supercoiling acros

88 erichia coli, and Mycobacterium tuberculosis gyrases and of heterologous enzymes reconstituted from s

89 cterial type II DNA topoisomerases (e.g. DNA gyrase) and are among the most important antibiotics in

90 ids in helix-4 of the target proteins, GyrA (gyrase) and ParC (topoisomerase IV).

91 of Escherichia coli derived gyrase versus Pa gyrase, and overexpression in the absence of antitoxin y

92 cies yet found to exist without a functional gyrase, and suggest an evolutionary path for generation

93 on; however, the activity and specificity of gyrase are augmented by a specialized DNA binding and wr

94 ing and the mechanical stress release due to gyrase are present in the system.

95 Bacterial gyrases are a class of type II topoisomerases that can i

96 ing domains (the C-terminal domains) of both gyrases are highly similar, both architecturally and in

97 We show that B. subtilis and E. coli gyrases are proficient DNA-stimulated ATPases and effici

98 roquinolone antibacterials, which target DNA gyrase, are critical agents used to halt the progression

99 ial agents that operate by inhibition of DNA gyrase as corroborated in an enzyme assay and by the inh

100 cleaved complexes with mutant GyrB-Cys(466) gyrase as evidenced by resistance to reversal by both ED

101 study suggested the inhibition of bacterial gyrase as the mechanism of action (MOA) of this chemical

102 inally annotated as potentially encoding DNA gyrase: ATGYRA, ATGYRB1, ATGYRB2, and ATGYRB3.

103 ar activity acting through inhibition of DNA Gyrase B (GyrB) ATPase.

104 , inhibitors of its ATP binding subunit, DNA gyrase B (GyrB), have so far not reached clinical use.

105 eport here the first cocrystal structures of gyrase B bound to coumermycin A1, revealing that one cou

106 zaindole ureas as a novel class of bacterial gyrase B inhibitors and detail the story of their evolut

107 6,7-tetrahydrobenzo[1,2-d]thiazole-based DNA gyrase B inhibitors, we replaced their central core with

108 were designed and prepared as potential DNA gyrase B inhibitors.

109 ther optimization of this novel class of DNA gyrase B inhibitors.

110 formed using multilocus sequence analysis of gyrase B of the beta subunit of DNA topoisomerase (gyrB)

111 acetic acid (24) in complex with E. coli DNA gyrase B revealed the binding mode of the inhibitor in t

112 with the gyrase A 'tower' and loop2 with the gyrase B TOPRIM domains.

113 rystal structure in complex with E. coli DNA gyrase B was obtained, revealing details of its binding

114 [4,5'-bithiazole]-2,2'-diamine inhibitors of gyrase B with a low micromolar inhibitory activity by im

115 icromolar inhibitors of Escherichia coli DNA gyrase based on the 5,6,7,8-tetrahydroquinazoline and 4,

116 atenated molecules become supercoiled by DNA gyrase before they undergo a complete decatenation by to

117 We identified an extended gyrase binding motif with phased 10-bp G/C content varia

118 Transcription can be resumed upon gyrase binding to the DNA segment.

119 g that bending ability of DNA contributes to gyrase binding.

120 hat fail to bind to its cellular target, DNA gyrase, but retain binding to the antitoxin, CcdA.

121 novobiocin resistance was not found to alter gyrase, but the ATPase that powers lipopolysaccharide (L

122 661 have been predicted to form a second DNA gyrase, but the reconstitute holoenzyme decatenated and

123 n orally active antibiotic that inhibits DNA gyrase by binding the ATP-binding site in the ATPase sub

124 road-spectrum antibacterials that target DNA gyrase by stabilizing DNA-cleavage complexes, but their

125 solution studies, shows that YacG represses gyrase by sterically occluding the principal DNA-binding

126 These results highlight a means by which gyrase can evolve distinct homeostatic supercoiling setp

127 pping to ATP turnover is why M. tuberculosis gyrase cannot supercoil DNA to the same extent as its ga

128 e closure of the N-gate is a key step in the gyrase catalytic cycle, as it captures the DNA segment t

129 DNA gyrase catalyzes ATP-dependent negative supercoiling of

130 ATP binding to the GyrB subunits of gyrase causes dimerization and N-gate closure.

131 argeted the GyrA subunit and stalled the DNA-gyrase cleavage complex.

132 on, the crystal structures of the WT Mtb DNA gyrase cleavage core and a fluoroquinolone-sensitized mu

133 cate, with single nucleotide resolution, DNA gyrase cleavage sites (GCSs) throughout the Escherichia

134 During catalysis, gyrase cleaves both DNA strands forming a covalently bou

135 Analysis of multiple DNA gyrase co-crystal structures, including asymmetric cleav

136 fusion truncate of Staphyloccocus aureus DNA gyrase complexed with DNA and diverse inhibitors have be

137 ion towards negative supercoiling, bacterial gyrase complexes bound to 137- or 217-bp DNA fragments r

138 Reverse gyrase comprises an N-terminal ATPase and a C-terminal t

139 ptional bursting depend on the intracellular gyrase concentration.

140 To address how gyrase copes with these topological challenges, we used

141 such compounds, 21 crystal structures of a "gyrase(CORE)" fusion truncate of Staphyloccocus aureus D

142 ous conformations sampled by these multiple "gyrase(CORE)" structures show rigid body movements of th

143 s-link between fluoroquinolone and GyrA-G81C gyrase correlated with exceptional bacteriostatic activi

144 oxicity required ATP, and it interfered with gyrase-dependent DNA supercoiling but not DNA relaxation

145 n bacteria is primarily caused by reversible gyrase dissociation from and rebinding to a DNA segment,

146 he structure of the 212 kDa Escherichia coli gyrase DNA binding and cleavage core containing this ins

147 NA and Top2a-DNA adducts in human cells, and gyrase-DNA adducts in Escherichia coli.

148 It is able to stabilize the transient DNA gyrase-DNA cleavage complex, a very efficient mode of ac

149 X-ray crystallography of DNA gyrase-DNA complexes shows the compounds binding to a pr

150 g mechanism involves the assembly of a large gyrase/DNA complex and conformational rearrangements cou

151 ther the A. thaliana genes encoded an active gyrase enzyme, nor whether that enzyme is indeed the tar

152 However, E. coli DNA gyrase essentially failed to negatively supercoil 35% st

153 ed in equipotent nanomolar inhibitors of DNA gyrase from Escherichia coli displaying improved inhibit

154 The IC50 values of compounds on DNA gyrase from Escherichia coli were in the low micromolar

155 both contribute to protection of E. coli DNA gyrase from quinolones.

156 ounds, the inhibitory activities against DNA gyrase from Staphylococcus aureus and topoisomerases IV

157 characterization of PcalRG, a novel reverse gyrase from the archaeon Pyrobaculum calidifontis.

158 erential regulatory effects of the C-tail in gyrases from different organisms.

159 Questions remain as to how gyrases from different species have evolved profound dif

160 CTD has a dramatic and unexpected impact on gyrase function.

161 , as the assay target, and expression of the gyrase gene (gyrB) as a normalizer, we were able to accu

162 before optimization, inhibitors of bacterial gyrase, GSK299423, ciprofloxacin, and etoposide exhibite

163 3 mutations in the target proteins-2 in DNA gyrase (GyrA) and 1 in topoisomerase IV (ParC), which oc

164 resulting from dual inhibition of bacterial gyrase (GyrB) and topoisomerase IV (ParE), and it demons

165 ubunits of the RNA polymerase (RpoB) and DNA gyrase (GyrB) and with the 16S rRNA-based phylogeny.

166 flagellin (flaB), and deoxyribonucleic acid gyrase (gyrB) genes and conducting a phylogenetic analys

167 Our observations demonstrate that gyrase has been modified in multiple ways throughout evo

168 nip Crinkle Virus1 subfamily of microrchidia Gyrase, Heat Shock Protein90, Histidine Kinase, MutL (GH

169 ted antagonist GSK299423) and remodeling the gyrase holoenzyme into an inactive, ATP-trapped configur

170 Strikingly, a "tail-less" gyrase holoenzyme is markedly impaired for DNA supercoil

171 In contrast, M. tuberculosis gyrase hydrolyzes ATP only slowly and is a poor supercoi

172 d- and chromosome-encoded homologues inhibit gyrase in a different manner than previously described a

173 marin antibiotics, compounds that target DNA gyrase in bacteria.

174 The lead compound inhibited DNA gyrase in gel-based assays, with an IC(50) of 3.16 +/- 1

175 ng the interactions of Qnr proteins with DNA gyrase in gram-negative bacteria.

176 with the relaxation-induced transcription of gyrase in other bacteria.

177 excellent targets for chemotherapy, and DNA gyrase in particular is a well-validated target for anti

178 cci clinical isolates and inhibit mutant DNA gyrase in-vitro.

179 ization of cleaved complex by N. gonorrhoeae gyrase increased in a fluoroquinolone-resistant mutant e

180 and reaches the activity of the B. subtilis gyrase, indicating that the activities of enzymes contai

181 oside's antibacterial activity is due to DNA gyrase inhibition and suggests other anticancer agents a

182 the ParE-type toxins, their reported role of gyrase inhibition utilized during plasmid-segregation ki

183 he activity of the SPTs was assessed for DNA gyrase inhibition, and the antibacterial activity across

184 nts and operate at least in part through DNA gyrase inhibition, leading to the accumulation of single

185 in activities including RNA scission and DNA gyrase inhibition.

186 we have previously demonstrated to be a DNA gyrase inhibitor in vitro, suggesting that ParE1/3 is li

187 Simocyclinone D8 (SD8), a potent DNA gyrase inhibitor made by Streptomyces antibioticus, is e

188 ls the export of simocyclinone, a potent DNA gyrase inhibitor made by Streptomyces antibioticus.

189 Simocyclinone D8 (SD8) is a potent DNA gyrase inhibitor produced by Streptomyces antibioticus T

190 re used to establish QC ranges for the novel gyrase inhibitor zoliflodacin against the ATCC strains r

191 n (transcription inhibitor), nalidixic acid (gyrase inhibitor), or A22 (MreB-cytoskeleton disruptor).

192 7-oxo-SD8 was essentially inactive as a DNA gyrase inhibitor, and the reduction of the keto group by

193 vitro, suggesting that ParE1/3 is likewise a gyrase inhibitor, despite its relatively low degree of s

194 Development of the DNA gyrase inhibitor, novobiocin, into a selective Hsp90 inh

195 D0914 upon removal of magnesium from the DNA-gyrase-inhibitor complex.

196 t of strains resistant to a variety of known gyrase inhibitors all exhibited sensitivity to ParE2.

197 bin inhibitors, HIV protease inhibitors, DNA gyrase inhibitors and many others.

198 (-)-1 was not cross-resistant with other DNA gyrase inhibitors such as fluoroquinolone and aminocouma

199 This novel class of DNA gyrase inhibitors was extensively investigated by variou

200 A series of gyrase inhibitors with known synthetic order formed the

201 l hits resulted in low nanomolar E. coli DNA gyrase inhibitors, some of which exhibited micromolar in

202 t aid in the development of species-specific gyrase inhibitors.

203 actors bind to and disrupt the quinolone-DNA-gyrase interaction is proposed.

204 -G81C gyrase, thereby revealing a novel drug-gyrase interaction not observed in crystal structures.

205 s basis we present a model for the AhQnr:DNA gyrase interaction where loop1 interacts with the gyrase

206 ays a functional role in mediating quinolone-gyrase interactions.

207 magnesium ion, which bridges fluoroquinolone-gyrase interactions.

208 Bacterial DNA gyrase introduces negative supercoils into chromosomal D

209 DNA gyrase is a bacterial DNA topoisomerase that catalyzes A

210 DNA gyrase is a clinically validated target for developing d

211 DNA gyrase is a DNA topoisomerase present in bacteria and pl

212 Reverse gyrase is a DNA topoisomerase specific for hyperthermoph

213 ith structural features present: B. subtilis gyrase is a minimal enzyme, and its subunits can functio

214 Gyrase is a molecular motor that harnesses the free ener

215 Gyrase is a type II DNA topoisomerase that introduces ne

216 Bacterial DNA gyrase is a well-established and validated target for th

217 Bacterial DNA gyrase is a well-known and validated target in the desig

218 TP during their reactions; however, only DNA gyrase is able to harness the free energy of hydrolysis

219 DNA gyrase is an essential bacterial enzyme required for the

220 An important antibiotic target, DNA gyrase is an essential bacterial enzyme that introduces

221 Results indicate that gyrase is better suited than topoisomerase IV to safely

222 The information about how gyrase is distributed along genomic DNA and whether its

223 Negative supercoiling by DNA gyrase is essential for maintaining chromosomal compacti

224 axation of negatively supercoiled DNA by DNA gyrase is inhibited, whereas the extent of supercoiling

225 Escherichia coli gyrase is known to favor supercoiling over decatenation,

226 DNA gyrase is the only type II topoisomerase in Mycobacteriu

227 The activity pattern of heterologous gyrases is in agreement with structural features present

228 RG is the most robust and processive reverse gyrase known to date; it is active over a wide range of

229 M. tuberculosis gyrase lacks a conserved serine that anchors a water-met

230 nal domains except the CTD squarely within a gyrase lineage, and the A. aeolicus GyrB subunit is capa

231 Gyrase maintained lower levels of cleavage complexes wit

232 also suggest that the wrapping mechanism of gyrase may have evolved to promote rapid removal of posi

233 By altering the superhelical density, gyrase may regulate expression of bacterial genes.

234 eaks, the antibacterial thiophenes stabilize gyrase-mediated DNA-cleavage complexes in either one DNA

235 Our assays confirmed PaParE inhibition of gyrase-mediated supercoiling of DNA with an IC(50) value

236 ochemical methods; i.e., DNA-nicking and DNA-gyrase methods to examine whether certain sequence-speci

237 The proposed gyrase model, with the DNA binding along the sides of th

238 We demonstrate that at least 300 gyrase molecules are stably bound to the chromosome at a

239 imes of ~2 s were observed for the dispersed gyrase molecules, which we propose maintain steady-state

240 gates were validated using the P. falciparum gyrase mRNA as a target (PfGyrA).

241 The DNA gyrase negative supercoiling mechanism involves the asse

242 The gyrases of many gram-negative bacteria harbor a 170-amin

243 indicate that the catalytic cycle of E. coli gyrase operates at high thermodynamic efficiency, and th

244 rase conflictingly categorized as either DNA gyrase or topo IV.

245 serine or acidic residue in the A subunit of gyrase or topoisomerase IV.

246 All gyrase orthologs rely on a homologous set of catalytic d

247 ted native lac is shown to be insensitive to Gyrase overexpression, even at critically low temperatur

248 DP (antitoxin CcdA) to its molecular target (gyrase poison CcdB).

249 However, in contrast to other gyrase poisons, ParE2 toxicity required ATP, and it inte

250 the QRDR of gyrA or gyrB; 1 did not have any gyrase polymorphisms.

251 In silico docking of indole on DNA gyrase predicts that indole docks perfectly to the ATP b

252 he cruciform and separation of the labels as gyrase progressively underwinds the DNA.

253 by unusual positive feedback control of the gyrase promoter and the temporal expression of three top

254 However, activation of the chlamydial gyrase promoter by increased supercoiling is unorthodox

255 Reverse gyrase reanneals denatured DNA and induces positive supe

256 The only exception is a gyrase reconstituted from mycobacterial GyrA and B. subt

257 time-resolved single-molecule measurements, gyrase relaxed overwound DNA with burst rates of approxi

258 Gyrase removed positive supercoils approximately 10-fold

259 Reverse gyrases (RGs) are the only topoisomerases capable of gen

260 In Escherichia coli topA strains, DNA gyrase selectively converts the positively supercoiled d

261 ts suggest for the first time that a reverse gyrase shares not only structural but also functional fe

262 rug etoposide with Staphylococcus aureus DNA gyrase, showing binding at the same sites in the cleaved

263 Gyrase struggled to bend or perhaps open a gap in DAP-su

264 e internal fragment of the gene encoding DNA gyrase subunit B (GyrB) for VGS species-level identifica

265 sequent adenylylation of its target, the DNA gyrase subunit GyrB.

266 uently showed that ATGYRB3 does not encode a gyrase subunit, the other three genes potentially encode

267 ific insertions in E. coli and mycobacterial gyrase subunits appear to prevent efficient functional i

268 iption inhibition leads to redistribution of gyrase suggesting that the enrichment is functionally si

269 set of BBZ compounds inhibited S. aureus DNA gyrase supercoiling activity with IC(50) values in the r

270 ach to develop a HT screen for inhibitors of gyrase supercoiling.

271 chanism of action, inhibiting the mutant DNA gyrase that confers FQR.

272 . thaliana encodes an organelle-targeted DNA gyrase that is the target of the quinolone drug ciproflo

273 ect on DNA-induced conformational changes of gyrase that precede strand passage and reduces DNA-stimu

274 main of the GyrA subunit of Escherichia coli gyrase (the 'CTD').

275 alanine (i.e., GyrA(A90)) in M. tuberculosis gyrase, the bridge still forms and plays a functional ro

276 We show here that, in contrast to E. coli gyrase, the C-tail is a very moderate negative regulator

277 identified over 40 compounds that target DNA gyrase, the cell wall, tryptophan, folate biosynthesis a

278 When gyrase, the sole T. thermophilus type II topoisomerase,

279 en with complexes formed by mutant GyrA-G81C gyrase, thereby revealing a novel drug-gyrase interactio

280 quinolone inhibition of Escherichia coli DNA gyrase, thus providing an appropriate model system for g

281 te through both inhibition of binding of DNA gyrase to DNA and accumulation of single-stranded DNA br

282 A production until it is bound by the enzyme gyrase to DNA, which releases the stress and allows for

283 DNA breaks, and by preventing the binding of gyrase to DNA.

284 n an ATP-independent reaction and works with gyrase to establish a topological equilibrium where supe

285 tance, analog 49c was found to be a dual DNA gyrase-topoisomerase IV inhibitor, with broad antibacter

286 -resistant to fluoroquinolones and other DNA gyrase/topoisomerase IV inhibitors used clinically.

287 inated the protective effect of QnrB1 on DNA gyrase toward inhibition by quinolones, whereas deletion

288 the DNA segment to be transported and poises gyrase toward strand passage.

289 of supercoiling activity of Escherichia coli gyrase upon deletion of the non-conserved acidic C-termi

290 The structures suggest that S. aureus gyrase uses a single moving-metal ion for cleavage and t

291 sis of high-speed structural dynamics of DNA gyrase using AuRBT revealed an unanticipated transient i

292 cious inhibition of Escherichia coli derived gyrase versus Pa gyrase, and overexpression in the absen

293 The mechanism of inhibition of DNA gyrase was distinct from the fluoroquinolones, as shown

294 ology, CT189/190 are the two subunits of DNA gyrase, whereas CT643 is a topoisomerase I.

295 eria utilize a unique type II topoisomerase, gyrase, which actively adds negative supercoils to chrom

296 fer from eukaryotes by having the enzyme DNA gyrase, which catalyses the ATP-dependent negative super

297 with the thermophile-specific enzyme reverse gyrase, which catalyzes positive supercoiling of DNA and

298 s a nanomolar inhibitor of the bacterial DNA gyrase with a strong activity against various Gram-negat

299 of antibacterial thiophenes that target DNA gyrase with a unique mechanism of action and have activi

300 ation of the quinolone-resistant A. thaliana gyrase yields active enzyme that is resistant to ciprofl