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