ライフサイエンスコーパス: gyrase

1 the detailed mechanism of SD8 inhibition of gyrase.

2 y Streptomyces antibioticus that targets DNA gyrase.

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

4 consistent with allosteric inhibition of DNA gyrase.

5 a bacterial topoisomerase, Escherichia coli gyrase.

6 kage by Streptococcus pneumoniae topo IV and gyrase.

7 been reported for Mycobacterium tuberculosis gyrase.

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

9 ling and DNA-stimulated ATPase activities of gyrase.

10 m of positive supercoil induction by reverse gyrase.

11 c cellular component, such as mRNA, DnaB, or gyrase.

12 validated drug targets such as bacterial DNA gyrase.

13 ATPase kinetics of Streptococcus pneumoniae gyrase.

14 s of the bacterial type II topoisomerase DNA gyrase.

15 n of the bacterial type-II topoisomerase DNA gyrase.

16 ynamic changes elicited by the inhibition of gyrase.

17 s and is a well-established inhibitor of DNA gyrase.

18 shown to inhibit the catalytic reactions of gyrase.

19 genes potentially encode subunits of a plant gyrase.

20 ant enzymes than moxifloxacin did against WT gyrase.

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

22 atalyzed by M. tuberculosis gyrase and other gyrases.

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

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

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

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

27 ixic acid to serve as a surrogate marker for gyrase A mutations associated with diminished fluoroquin

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

29 he N-terminal domain of the Escherichia coli gyrase A subunit and simocyclinone D8, revealing two bin

30 Gyrase, a prokaryotic heterotetrameric type IIA topo, in

31 Gyrase, a prokaryotic type IIA topoisomerase, consumes A

32 agents that act by inhibiting bacterial DNA gyrase, a target of clinical significance.

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

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

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

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

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

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

39 rate negative regulator of Bacillus subtilis gyrase activity.

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

41 we detected catenation was 50-60 bp for DNA gyrase and 40 bp for topoisomerase IV (Topo IV).

42 ssage of two type IA topoisomerases: reverse gyrase and a protein complex of topoisomerase III alpha

43 In the presence of gyrase and ATP, we observe bursts of rotation correspond

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

45 ing DNA supercoiling by Escherichia coli DNA gyrase and DNA relaxation by eukaryotic topoisomerases I

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

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

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

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

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

51 Escherichia coli gyrase and human topoisomerase IIalpha were challenged w

52 antibiotic fluoroquinolone by binding to DNA gyrase and inhibiting its activity.

53 MfpA binds to DNA gyrase and inhibits its activity.

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

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

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

57 The ability of changes in both gyrase and quinolone structure to enhance protein synthe

58 2+) has a regulatory role in M. tuberculosis gyrase and suggest a model for the modulation of gyrase

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

60 nt in the transcribed track and suggests how gyrase and TopA control upstream and downstream transcri

61 tly possess two type IIA DNA topoisomerases, gyrase and topo IV, which maintain chromosome topology b

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

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

64 They are inhibitors of bacterial gyrase and topoisomerase IV and demonstrate clinically u

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

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

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

68 Bacterial DNA gyrase and topoisomerase IV are well-characterized clini

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

70 DNA gyrase and topoisomerase IV control bacterial DNA topolo

71 Bacterial DNA gyrase and topoisomerase IV control the topological stat

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

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

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

75 Although bacterial gyrase and topoisomerase IV have critical interactions w

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

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

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

79 ow molecular weight, synthetic inhibitors of gyrase and topoisomerase IV that bind to the ATP sites a

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

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

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

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

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

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

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

87 inhibitory activities against S. aureus DNA gyrase and topoisomerase IV, with weak activity against

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

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

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

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

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

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

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

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

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

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

98 sical interaction between GyrA, subunit A of gyrase, and MarR, a repressor of the marRAB operon.

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

100 floxacin, a fluoroquinolone inhibitor of DNA gyrase, and to topoisomerase IV and were almost complete

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

102 ibiotics novobiocin and clorobiocin with DNA gyrase are illustrative of the importance of bound water

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

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

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

106 Members of one class of the enzymes, DNA gyrases, are configured to carry out an intramolecular r

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

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

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

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

111 activity against gram-positive pathogens, no gyrase ATPase activity from a gram-positive organism is

112 eal unique features of the S. pneumoniae DNA gyrase ATPase and demonstrate the utility of the assay f

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

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

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

116 6,7-tetrahydrobenzo[1,2-d]thiazole-based DNA gyrase B inhibitors, we replaced their central core with

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

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

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

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

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

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

123 [4,5'-bithiazole]-2,2'-diamine inhibitors of gyrase B with a low micromolar inhibitory activity by im

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

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

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

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

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

129 661 have been predicted to form a second DNA gyrase, but the reconstitute holoenzyme decatenated and

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

131 ional antibiotics that inhibit bacterial DNA gyrase by preventing DNA binding to the enzyme.

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

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

134 report here several activities that reverse gyrase can efficiently mediate with a substoichiometric

135 of bubble substrate demonstrate that reverse gyrase can function as a DNA renaturase.

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

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

138 DNA gyrase catalyzes ATP-dependent negative supercoiling of

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

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

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

142 B has been previously shown to stabilize the gyrase 'cleavage complex', but it has not been shown to

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

144 Covalent topoisomerase I and DNA gyrase complexes are converted into double-strand breaks

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

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

147 ptional bursting depend on the intracellular gyrase concentration.

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

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

150 erium Streptococcus pneumoniae, and promotes gyrase-dependent single- and double-stranded DNA cleavag

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

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

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

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

155 xplained by drug-mediated destabilization of gyrase-DNA complexes.

156 enzyme inhibition in which the -1 nt at the gyrase-DNA gate exhibit different CL reactivities to pro

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

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

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

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

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

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

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

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

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

166 anscriptional responses to the modulation of gyrase function have identified two types of topoisomera

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

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

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

170 CL did not induce cleavage by a mutant gyrase (GyrA G79A) identified here in CL-resistant pneum

171 encing of the gene encoding subunit A of DNA gyrase (gyrA) revealed a mutation associated with fluoro

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

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

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

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

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

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

178 ique ATP-binding Bergerat fold with the GHL (gyrase, Hsp90, and MutL) family of proteins.

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

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

181 rial drugs such as nalidixic acid target DNA gyrase in Escherichia coli.

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

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

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

185 Here we observe the activity of gyrase in real time by tracking the rotation of a submic

186 tablish by genetic means that CL targets DNA gyrase in the gram-positive bacterium Streptococcus pneu

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

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

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

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

191 in activities including RNA scission and DNA gyrase inhibition.

192 itor covalently connected to a topoisomerase/gyrase inhibitor are described.

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

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

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

196 of the former gene, as well as using the DNA gyrase inhibitor novobiocin.

197 Simocyclinone D8 is a potent DNA gyrase inhibitor produced by Streptomyces antibioticus T

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

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

200 e C4, which is essentially inactive as a DNA gyrase inhibitor, also induces simX expression in vivo a

201 7-oxo-SD8 was essentially inactive as a DNA gyrase inhibitor, and the reduction of the keto group by

202 Novobiocin, a known DNA gyrase inhibitor, binds to a nucleotide-binding site loc

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

204 Recent studies have shown that the DNA gyrase inhibitor, novobiocin, binds to a previously unre

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

206 The DNA gyrase inhibitor, novobiocin, was recently shown to inhi

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

208 tracyclines, clindamycin and macrolides) and gyrase inhibitors (such as ciprofloxacin) cause modest a

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

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

211 (-)-1 was not cross-resistant with other DNA gyrase inhibitors such as fluoroquinolone and aminocouma

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

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

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

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

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

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

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

219 magnesium ion, which bridges fluoroquinolone-gyrase interactions.

220 DNA gyrase is a clinically validated target for developing d

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

222 Reverse gyrase is a DNA topoisomerase specific for hyperthermoph

223 DNA gyrase is a molecular machine that uses the energy of AT

224 Gyrase is a molecular motor that harnesses the free ener

225 Gyrase is a type II DNA topoisomerase that introduces ne

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

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

228 Reverse gyrase is able to anneal single strands, thereby increas

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

230 DNA gyrase is an essential bacterial enzyme required for the

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

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

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

234 Inhibition of the ATPase activity of DNA gyrase is the mechanism by which coumarin-class antibiot

235 DNA gyrase is the only topoisomerase able to introduce negat

236 DNA gyrase is the only type II topoisomerase in Mycobacteriu

237 When DNA gyrase is trapped on bacterial chromosomes by quinolone

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

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

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

241 Gyrase maintained lower levels of cleavage complexes wit

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

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

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

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

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

247 The DNA gyrase negative supercoiling mechanism involves the asse

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

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

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

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

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

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

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

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

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

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

258 esulting in an A271E substitution in the DNA gyrase protein generated a strain unable to grow on the

259 ent covalent protein-DNA intermediate in the gyrase reaction cycle, referred to as the cleavage compl

260 Reverse gyrase reanneals denatured DNA and induces positive supe

261 none D8 are comparatively weak inhibitors of gyrase relative to the parent compound, but their combin

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

263 Gyrase removed positive supercoils approximately 10-fold

264 t efficient positive supercoiling by reverse gyrase requires a bubble size larger than 20 nucleotides

265 yme as relaxed circular DNA treated with DNA gyrase, resulted in the highest levels of ATPase activit

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

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

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

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

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

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

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

273 eady-state changes elicited by a mutation in gyrase, such as the D82G mutation in GyrA, and (ii) dyna

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

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

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

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

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

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

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

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

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

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

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

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

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

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 DNA gyrase uses the energy of ATP hydrolysis to introduce ne

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

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

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

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

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

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

297 nteracts directly with the target enzyme DNA gyrase, which is a validated drug target.

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