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1 laxing enzyme (eukaryotic topoisomerase I or DNA gyrase).
2 ugh validated drug targets such as bacterial DNA gyrase.
3 itors of the bacterial type II topoisomerase DNA gyrase.
4 ition of the bacterial type-II topoisomerase DNA gyrase.
5 otics and is a well-established inhibitor of DNA gyrase.
6 emic negative supercoil energy introduced by DNA gyrase.
7 is the pharmacophore for targeting bacterial DNA gyrase.
8 at minimally contained T7 RNA polymerase and DNA gyrase.
9 cent of those seen in structures of MutL and DNA gyrase.
10 h are the putative target binding motifs for DNA gyrase.
11 coumermycin A1, an antibiotic that inhibits DNA gyrase.
12 t interacts with the target bacterial enzyme DNA gyrase.
13 e; the putative target of this antibiotic is DNA gyrase.
14 for clinically useful antibiotics that block DNA gyrase.
15 a interaction with the type II topoisomerase DNA gyrase.
16 elated to the ATP-binding motif of bacterial DNA gyrase.
17 the spirochete and functions as a subunit of DNA gyrase.
18 l environment via changes in the activity of DNA gyrase.
19 CcdB is a bacterial toxin that targets DNA gyrase.
20 ed within the gene encoding the A subunit of DNA gyrase.
21 to that of an ATPase-containing fragment of DNA gyrase.
22 r protein CcdB with its intracellular target DNA gyrase.
23 ts and were found to be potent inhibitors of DNA gyrase.
24 the amino acid sequence of the A subunit of DNA gyrase.
25 in mapped in gyrB, one of the genes encoding DNA gyrase.
26 e quinolone group of antibacterial agents is DNA gyrase.
27 lly modified peptide that inhibits bacterial DNA gyrase.
28 rs, consistent with allosteric inhibition of DNA gyrase.
29 ed by Streptomyces antibioticus that targets DNA gyrase.
30 Against Gram-negative microorganisms and DNA gyrase a preference for S-absolute configuration was
31 complexed with the N-terminal domain of the DNA gyrase A protein (GyrA) suggested that four SD8 mole
34 d in terms of current mechanistic models for DNA gyrase action and the possible in vivo roles of the
35 ion, the reaction selectivity for a model of DNA gyrase action that assumes existence of a free loop
36 yrI (also called sbmC) gene product inhibits DNA gyrase activity in vitro, while the rob protein appe
37 fective for the DNA relaxation activity, and DNA gyrase activity is reduced; second, the suppressor p
38 chemical network) resulting in inhibition of DNA gyrase activity, the primary target of fluoroquinolo
41 hich we detected catenation was 50-60 bp for DNA gyrase and 40 bp for topoisomerase IV (Topo IV).
42 d both inhibit bacterial growth by attacking DNA gyrase and by stimulating enzyme-induced breaks in b
43 omal gyrB gene that encodes the B subunit of DNA gyrase and confers resistance to the antibiotic coum
44 cdB can stabilise a cleavage complex between DNA gyrase and DNA in a manner distinct from quinolones
45 ssaying DNA supercoiling by Escherichia coli DNA gyrase and DNA relaxation by eukaryotic topoisomeras
46 agent in complex with Staphylococcus aureus DNA gyrase and DNA, showing a new mode of inhibition tha
47 y and explains both its inhibitory effect on DNA gyrase and fluoroquinolone resistance resulting from
48 nds were tested for their ability to inhibit DNA gyrase and found to exhibit significant reduction in
50 f the bgl operon occur in the genes encoding DNA gyrase and in the gene encoding the nucleoid associa
54 as a molecular 'clamp' mechanism, similar to DNA gyrase and MutL, whose opening and closing by transi
56 h rate but bind to different target enzymes (DNA gyrase and penicillin-binding proteins, respectively
60 acteria possess two type IIA topoisomerases, DNA gyrase and topo IV, that together help manage chromo
63 Quinolone antimicrobial drugs target both DNA gyrase and topoisomerase IV (Topo IV) and convert th
69 YejK interacts with all the subunits of both DNA gyrase and topoisomerase IV and has measurable effec
70 /ParE ATP-binding sites located on bacterial DNA gyrase and topoisomerase IV and not utilized by mark
76 mpound 27 was the most balanced inhibitor of DNA gyrase and topoisomerase IV from both E. coli and S.
79 rahydropyran-based molecules that are potent DNA gyrase and topoisomerase IV inhibitors and display e
80 for structure-based optimization toward dual DNA gyrase and topoisomerase IV inhibitors with antibact
81 this class of compounds toward balanced dual DNA gyrase and topoisomerase IV inhibitors with antibact
83 ibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) are of interest for the
84 ibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) display potent activity
85 ibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) display potent antibact
86 ibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) have the potential to b
87 n of a new class of bacterial topoisomerase (DNA gyrase and topoisomerase IV) inhibitors binding in t
88 organisms, (b) inhibitory activities against DNA gyrase and topoisomerase IV, and (c) no inhibitory a
89 floxacin, inhibit the type 2 topoisomerases, DNA gyrase and topoisomerase IV, and can cleave DNA at s
90 ch as 6 and 21 are potent inhibitors of both DNA gyrase and topoisomerase IV, displaying antibacteria
91 rong inhibitory activities against S. aureus DNA gyrase and topoisomerase IV, with weak activity agai
96 ary phase, whereas during exponential growth DNA gyrase and/or transcription equalizes supercoiling a
97 t bacterial type II DNA topoisomerases (e.g. DNA gyrase) and are among the most important antibiotics
98 related with excess negative supercoiling by DNA gyrase, and the gyrase inhibitor, coumermycin, rever
99 to ofloxacin, a fluoroquinolone inhibitor of DNA gyrase, and to topoisomerase IV and were almost comp
100 antibiotics novobiocin and clorobiocin with DNA gyrase are illustrative of the importance of bound w
102 Fluoroquinolone antibacterials, which target DNA gyrase, are critical agents used to halt the progres
104 cterial agents that operate by inhibition of DNA gyrase as corroborated in an enzyme assay and by the
106 reveal unique features of the S. pneumoniae DNA gyrase ATPase and demonstrate the utility of the ass
108 ever, inhibitors of its ATP binding subunit, DNA gyrase B (GyrB), have so far not reached clinical us
109 4,5,6,7-tetrahydrobenzo[1,2-d]thiazole-based DNA gyrase B inhibitors, we replaced their central core
112 cture of the 43 kDa N-terminal domain of the DNA gyrase B protein (GyrB) shows that the majority of t
113 Glu in the highly conserved QTK-loop in the DNA gyrase B protein homologous domain of Drosophila top
115 N-terminal fragment of the Escherichia coli DNA gyrase B protein in complexes with two different inh
116 ure of the 43 kDa N-terminal fragment of the DNA gyrase B protein shows a large cavity within the pro
117 -oxoacetic acid (24) in complex with E. coli DNA gyrase B revealed the binding mode of the inhibitor
118 on crystal structure in complex with E. coli DNA gyrase B was obtained, revealing details of its bind
120 ow micromolar inhibitors of Escherichia coli DNA gyrase based on the 5,6,7,8-tetrahydroquinazoline an
121 se catenated molecules become supercoiled by DNA gyrase before they undergo a complete decatenation b
122 nt) sequence of the Treponema denticola (Td) DNA gyrase beta-subunit gene (gyrB) has been determined.
123 elegans homologues of pyruvate carboxylase, DNA gyrase, beta-adrenergic receptor kinase, and human h
126 atalytic domain across the DNA gate, whereas DNA gyrase binds to DNA not only at the amino-terminal c
128 dB that fail to bind to its cellular target, DNA gyrase, but retain binding to the antitoxin, CcdA.
129 660/661 have been predicted to form a second DNA gyrase, but the reconstitute holoenzyme decatenated
130 is an orally active antibiotic that inhibits DNA gyrase by binding the ATP-binding site in the ATPase
131 mutants, second, the specific inhibition of DNA gyrase by novobiocin, and third, the genetic removal
132 and coumermycin A(1) target the B subunit of DNA gyrase by presentation of the 5-methyl-pyrrolyl-2-ca
133 unctional antibiotics that inhibit bacterial DNA gyrase by preventing DNA binding to the enzyme.
134 re broad-spectrum antibacterials that target DNA gyrase by stabilizing DNA-cleavage complexes, but th
135 ported specific labeling of Escherichia coli DNA gyrase by the ATP affinity analog pyridoxal 5'-dipho
137 imidodiphosphate (ADPNP) to Escherichia coli DNA gyrase can lead to a limited noncatalytic supercoili
140 action, the crystal structures of the WT Mtb DNA gyrase cleavage core and a fluoroquinolone-sensitize
143 at inhibition occurs specifically at the DNA-DNA gyrase complex and is not attributable to nonspecifi
144 ic acid monohydroxamides can bind to the DNA-DNA gyrase complex in a similar fashion as that hypothes
146 rentiate between the C-terminus of Hsp90 and DNA gyrase, converted a well-established gyrase inhibito
148 wo indispensable type II DNA topoisomerases, DNA gyrase encoded by gyrB and gyrA and topoisomerase IV
150 sulted in equipotent nanomolar inhibitors of DNA gyrase from Escherichia coli displaying improved inh
154 compounds, the inhibitory activities against DNA gyrase from Staphylococcus aureus and topoisomerases
156 ication of a 176-base pair fragment from the DNA gyrase gene of Neisseria gonorrhoeae was performed a
157 Quinolone antibacterial drugs target both DNA gyrase (Gyr) and topoisomerase IV (Topo IV) and form
159 Sequencing of the gene encoding subunit A of DNA gyrase (gyrA) revealed a mutation associated with fl
160 ta subunits of the RNA polymerase (RpoB) and DNA gyrase (GyrB) and with the 16S rRNA-based phylogeny.
163 of drug-DNA interaction in the A subunit of DNA gyrase has previously been identified from crystallo
164 Earlier results, however, indicated that DNA gyrase has the primary role in unlinking the catenat
168 Because the primary target of quinolones is DNA gyrase in Gram-negative strains, we tested the abili
169 are excellent targets for chemotherapy, and DNA gyrase in particular is a well-validated target for
171 e establish by genetic means that CL targets DNA gyrase in the gram-positive bacterium Streptococcus
174 emonstrated that novobiocin, an inhibitor of DNA gyrase, inhibited in vitro DNA replication by preven
176 etoposide's antibacterial activity is due to DNA gyrase inhibition and suggests other anticancer agen
177 agents and operate at least in part through DNA gyrase inhibition, leading to the accumulation of si
178 ine whether these moieties are important for DNA gyrase inhibition, these compounds were tested for t
180 hich we have previously demonstrated to be a DNA gyrase inhibitor in vitro, suggesting that ParE1/3 i
182 ntrols the export of simocyclinone, a potent DNA gyrase inhibitor made by Streptomyces antibioticus.
186 inone C4, which is essentially inactive as a DNA gyrase inhibitor, also induces simX expression in vi
187 7-oxo-SD8 was essentially inactive as a DNA gyrase inhibitor, and the reduction of the keto grou
188 transcription is inhibited by novobiocin, a DNA gyrase inhibitor, at concentrations subinhibitory fo
197 an smc null mutant was hypersensitive to the DNA gyrase inhibitors coumermycin A1 and norfloxacin.
198 ly, (-)-1 was not cross-resistant with other DNA gyrase inhibitors such as fluoroquinolone and aminoc
200 itial hits resulted in low nanomolar E. coli DNA gyrase inhibitors, some of which exhibited micromola
201 this basis we present a model for the AhQnr:DNA gyrase interaction where loop1 interacts with the gy
215 se ATP during their reactions; however, only DNA gyrase is able to harness the free energy of hydroly
218 al product antibiotics that target bacterial DNA gyrase is assembled from tyrosine by nonribosomal pe
219 nation and the introduction of supercoils by DNA gyrase is discussed in the context of the simulation
220 the dimerization domain of the B subunit of DNA gyrase is fused to the cytoplasmic domain of VEGFRs
221 Relaxation of negatively supercoiled DNA by DNA gyrase is inhibited, whereas the extent of supercoil
222 ed circular DNA templates in the presence of DNA gyrase is known to stimulate negative DNA supercoili
231 o biochemical methods; i.e., DNA-nicking and DNA-gyrase methods to examine whether certain sequence-s
233 t, the utilization of topoisomerase I and/or DNA gyrase mutants, second, the specific inhibition of D
234 fferent inhibitors of the ATPase activity of DNA gyrase, namely the coumarin antibiotic, novobiocin,
237 he synthesis and inhibitory activity against DNA gyrase of a series of diphenic acid monohydroxamides
238 t study has analysed the action of bacterial DNA gyrase on a single substrate DNA molecule, discrimin
239 strains or drugs that specifically inhibited DNA gyrase or bound to DNA directly, thereby affecting c
240 s either by interfering with the activity of DNA gyrase or by facilitating the relaxation reaction.
241 was mostly normal in cells with inactivated DNA gyrase or in mukB-null mutants lacking topA, althoug
243 ight inhibit transcription, DNA replication, DNA gyrase or topoisomerase I; however, we found no furt
245 f both forks required the presence of either DNA gyrase or topoisomerase IV, suggesting that modulati
246 le resulting in an A271E substitution in the DNA gyrase protein generated a strain unable to grow on
249 enzyme as relaxed circular DNA treated with DNA gyrase, resulted in the highest levels of ATPase act
251 er drug etoposide with Staphylococcus aureus DNA gyrase, showing binding at the same sites in the cle
252 ine-naphthyridine agents, which target novel DNA gyrase sites, other novel quinolones that have high
253 otide internal fragment of the gene encoding DNA gyrase subunit B (GyrB) for VGS species-level identi
254 n reading frame with significant homology to DNA gyrase subunit B (gyrB) of Helicobacter pylori.
256 eviously reported experiments, inhibition of DNA gyrase supercoiling activity by wild-type MccB17 als
257 subset of BBZ compounds inhibited S. aureus DNA gyrase supercoiling activity with IC(50) values in t
258 example in which misfolding of one protein, DNA gyrase, suppresses a deficiency of another, topoisom
259 nt N78 are homologous to two key residues of DNA gyrase that affect quinolone sensitivity, we generat
261 at A. thaliana encodes an organelle-targeted DNA gyrase that is the target of the quinolone drug cipr
263 tenation activity of Topo IV but not that of DNA gyrase, the other type II topoisomerase in the cell.
264 ves quinolone inhibition of Escherichia coli DNA gyrase, thus providing an appropriate model system f
265 de a physical explanation for the ability of DNA gyrase to constrain a positive superhelical DNA wrap
266 perate through both inhibition of binding of DNA gyrase to DNA and accumulation of single-stranded DN
267 ch corresponds to the A subunit of bacterial DNA gyrase, to identify amino acid side chains that augm
268 instance, analog 49c was found to be a dual DNA gyrase-topoisomerase IV inhibitor, with broad antiba
269 mutations in the gyrA and parC genes of the DNA gyrase/topoisomerase IV complex that occurred in the
270 eliminated the protective effect of QnrB1 on DNA gyrase toward inhibition by quinolones, whereas dele
273 nalysis of high-speed structural dynamics of DNA gyrase using AuRBT revealed an unanticipated transie
274 e have analysed the DNA cleavage reaction of DNA gyrase using oligonucleotides annealed to a single-s
276 rase IV were efficient at this task, whereas DNA gyrase was very inefficient at precatenane removal.
277 in sequence to the GyrA and GyrB subunits of DNA gyrase, we have used DNA sequence analysis to identi
280 n both parC (DNA topoisomerase IV) and gyrA (DNA gyrase), which were shown previously to confer fluor
281 differ from eukaryotes by having the enzyme DNA gyrase, which catalyses the ATP-dependent negative s
284 The C-terminal domain of the A subunit of DNA gyrase, which we term Gac, is naturally synthesized
285 in is a nanomolar inhibitor of the bacterial DNA gyrase with a strong activity against various Gram-n
286 lass of antibacterial thiophenes that target DNA gyrase with a unique mechanism of action and have ac
287 a biochemical analysis of the interaction of DNA gyrase with the Mu SGS, pSC101 and pBR322 sites.
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