PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 2831608-2 1988 For many of the quinolone agents, increased antibacterial potency correlates with increased potency in inhibiting the essential bacterial enzyme DNA gyrase. Quinolones 16-25 DNA topoisomerase II alpha Homo sapiens 145-155 2549608-1 1989 Recent studies concerning the mechanism of action of quinolones against DNA gyrase are reviewed. Quinolones 53-63 DNA topoisomerase II alpha Homo sapiens 72-82 2549608-2 1989 DNA gyrase is an essential bacterial enzyme known to be a primary target of quinolone agents. Quinolones 76-85 DNA topoisomerase II alpha Homo sapiens 0-10 2549608-3 1989 Quinolone-resistant alleles of both the gyrA and gyrB genes of DNA gyrase have been sequenced, and domains that affect the action of quinolones have been identified within the amino terminus of the gyrase A peptide and the midportion of the gyrase B peptide. Quinolones 0-9 DNA topoisomerase II alpha Homo sapiens 63-73 2549608-3 1989 Quinolone-resistant alleles of both the gyrA and gyrB genes of DNA gyrase have been sequenced, and domains that affect the action of quinolones have been identified within the amino terminus of the gyrase A peptide and the midportion of the gyrase B peptide. Quinolones 133-143 DNA topoisomerase II alpha Homo sapiens 63-73 2549608-4 1989 In addition, an ATP-induced structural transition of DNA complexed with DNA gyrase was shown to be blocked by norfloxacin, but the means by which quinolones effect this change and the molecular site of quinolone binding remain unclear. Quinolones 146-156 DNA topoisomerase II alpha Homo sapiens 72-82 2549608-4 1989 In addition, an ATP-induced structural transition of DNA complexed with DNA gyrase was shown to be blocked by norfloxacin, but the means by which quinolones effect this change and the molecular site of quinolone binding remain unclear. Quinolones 146-155 DNA topoisomerase II alpha Homo sapiens 72-82 2549608-5 1989 Studies of structure-activity relationships of the quinolone molecule have been expanded and have included effects of quinolones on DNA gyrase. Quinolones 118-128 DNA topoisomerase II alpha Homo sapiens 132-142 2546584-0 1989 Mechanism of inhibition of DNA gyrase by quinolone antibacterials: specificity and cooperativity of drug binding to DNA. Quinolones 41-50 DNA topoisomerase II alpha Homo sapiens 27-37 2546584-1 1989 Although the functional target of quinolone antibacterials such as nalidixic acid and norfloxacin has been identified as the enzyme DNA gyrase, the direct binding site of the drug is the DNA molecule [Shen, L. L., & Pernet, A. G. (1985) Proc. Quinolones 34-43 DNA topoisomerase II alpha Homo sapiens 132-142 2546585-0 1989 Mechanism of inhibition of DNA gyrase by quinolone antibacterials: a cooperative drug--DNA binding model. Quinolones 41-50 DNA topoisomerase II alpha Homo sapiens 27-37 2546585-1 1989 We have proposed a cooperative quinolone-DNA binding model for the inhibition of DNA gyrase. Quinolones 31-40 DNA topoisomerase II alpha Homo sapiens 81-91 2536729-0 1989 Mechanism of quinolone inhibition of DNA gyrase. Quinolones 13-22 DNA topoisomerase II alpha Homo sapiens 37-47 3293157-8 1988 Resistance mediated by mutations in genes altering DNA gyrase and expression of outer membrane proteins has been described for ciprofloxacin and other quinolones. Quinolones 151-161 DNA topoisomerase II alpha Homo sapiens 51-61 3279489-10 1988 Quinolones inhibit the bacterial enzyme DNA gyrase. Quinolones 0-10 DNA topoisomerase II alpha Homo sapiens 40-50 3008075-4 1986 The quinolones interfere with bacterial DNA transcription by inhibiting the enzyme DNA gyrase, that so far has only been found in bacteria. Quinolones 4-14 DNA topoisomerase II alpha Homo sapiens 83-93 2829716-1 1987 The Computer Automated Structure Evaluation (CASE) program was used to study a series of quinolone antibacterial agents for which experimental data pertaining to DNA gyrase inhibition as well as MICs against several strains of gram-positive and gram-negative bacteria are available. Quinolones 89-98 DNA topoisomerase II alpha Homo sapiens 162-172 3008075-5 1986 The nature of the activity of the quinolones on DNA gyrase makes it highly unlikely that resistance is carried on plasmids. Quinolones 34-44 DNA topoisomerase II alpha Homo sapiens 48-58 26055367-2 2015 Both target host DNA gyrase, as do quinolones and plasmid-determined Qnr proteins that protect gyrase from quinolone inhibition. Quinolones 35-45 DNA topoisomerase II alpha Homo sapiens 17-27 31683749-2 2019 The new hybrids were intended to have a new binding mode to DNA gyrase, that will allow for a more potent antibacterial effect, and for activity against current quinolone-resistant bacterial strains. Quinolones 161-170 DNA topoisomerase II alpha Homo sapiens 60-70 3019897-4 1986 Inhibition of DNA gyrase by quinolones and possible effects on the structure of DNA are reviewed. Quinolones 28-38 DNA topoisomerase II alpha Homo sapiens 14-24 27132191-2 2016 In the majority of these cases, resistance to fluoroquinolone-based antibiotics is associated with genetic mutations in the quinolone resistance-determining region (QRDR) of the bacterial DNA gyrase gene gyrA. Quinolones 52-61 DNA topoisomerase II alpha Homo sapiens 188-198 26239981-1 2015 Qnr is a plasmid-encoded and chromosomally determined protein that protects DNA gyrase and topoisomerase IV from inhibition by quinolones. Quinolones 127-137 DNA topoisomerase II alpha Homo sapiens 76-86 26243148-1 2015 This study aimed to investigate the role of quinolone resistance-determining regions (QRDRs) of DNA gyrase (encoded by gyrA and gyrB) and topoisomerase IV (encoded by parC and parE) associated with fluoroquinolone resistance. Quinolones 44-53 DNA topoisomerase II alpha Homo sapiens 96-106 25343976-4 2014 DNA gyrase-targeting pentapeptide repeat proteins can both inhibit DNA gyrase-a potentially useful therapeutic property-and contribute to resistance to quinolone antibacterials (by acting to prevent them forming a lethal complex with the DNA and enzyme). Quinolones 152-161 DNA topoisomerase II alpha Homo sapiens 0-10 25343976-4 2014 DNA gyrase-targeting pentapeptide repeat proteins can both inhibit DNA gyrase-a potentially useful therapeutic property-and contribute to resistance to quinolone antibacterials (by acting to prevent them forming a lethal complex with the DNA and enzyme). Quinolones 152-161 DNA topoisomerase II alpha Homo sapiens 67-77 23008691-1 2011 BACKGROUND AND THE PURPOSE OF THE STUDY: Ofloxacin is a quinolone synthetic antibiotic, which acts against resistant mutants of bacteria by inhibiting DNA gyrase. Quinolones 56-65 DNA topoisomerase II alpha Homo sapiens 151-161 22838215-9 2012 The main mechanism is considered to be linked with mutations in the quinolone-resistance determining region (QRDR) of the target genes (gyrA and gyrB encoding DNA gyrase, and parC and parE encoding topoisomerase IV). Quinolones 68-77 DNA topoisomerase II alpha Homo sapiens 159-169 17310788-1 2006 Fluoroquinolones are present considered as an important independent group of chemotherapeutics within the class of quinolones, DNA-gyrase inhibitors characterized by high clinical efficacy and numerous indications, and clinical efficacy and humerous indications, and are known as a serious alternative to other highly efficient broad spectrum antibiotics. Quinolones 6-16 DNA topoisomerase II alpha Homo sapiens 127-137 17008172-4 2006 The Qnr proteins, capable of protecting DNA gyrase from quinolones, have homologues in water-dwelling bacteria, and seem to have been in circulation for some time, having achieved global distribution in a variety of plasmid environments and bacterial genera. Quinolones 56-66 DNA topoisomerase II alpha Homo sapiens 40-50 12019094-0 2002 Quinolone-binding pocket of DNA gyrase: role of GyrB. Quinolones 0-9 DNA topoisomerase II alpha Homo sapiens 28-38 14502475-6 2003 Examples of this methodology are illustrated using QSAR equations developed for the inhibition of quinolone-resistant bacterial DNA gyrase and human topoisomerase-II inhibition by a series of quinolone antibacterial agents. Quinolones 98-107 DNA topoisomerase II alpha Homo sapiens 128-138 14502475-6 2003 Examples of this methodology are illustrated using QSAR equations developed for the inhibition of quinolone-resistant bacterial DNA gyrase and human topoisomerase-II inhibition by a series of quinolone antibacterial agents. Quinolones 192-201 DNA topoisomerase II alpha Homo sapiens 128-138 12624075-0 2003 Identification of mycobacterial species by PCR sequencing of quinolone resistance-determining regions of DNA gyrase genes. Quinolones 61-70 DNA topoisomerase II alpha Homo sapiens 105-115 12624075-1 2003 The determination of the amino acid sequence of quinolone resistance-determining regions (QRDRs) in the A and B subunits of DNA gyrase is the molecular test for the detection of fluoroquinolone resistance in mycobacteria. Quinolones 48-57 DNA topoisomerase II alpha Homo sapiens 124-134 12558069-1 2003 The quinolones are a potent group of drugs that target the essential bacterial enzymes DNA gyrase and topoisomerase IV. Quinolones 4-14 DNA topoisomerase II alpha Homo sapiens 87-97 12019094-1 2002 DNA gyrase is a prokaryotic type II topoisomerase and a major target of quinolone antibacterials. Quinolones 72-81 DNA topoisomerase II alpha Homo sapiens 0-10 12540265-3 2001 In addition, this unique peptide DNA gyrase inhibitor provides a contrast in activity versus quinolones, Ca(2+)-mediated inhibition/cleavage and the bacterial toxin/peptide CcdB. Quinolones 93-103 DNA topoisomerase II alpha Homo sapiens 33-43 12582434-1 2002 In order to produce their cytotoxic effect, quinolones must enter the cell through the bacterial membrane to reach their target, DNA-gyrase or topoisomerase IV, and induce cell death. Quinolones 44-54 DNA topoisomerase II alpha Homo sapiens 129-139 11427730-2 2001 MccB17 inhibits its cellular target, DNA gyrase, by trapping the enzyme in a complex that is covalently bound to double-strand cleaved DNA, in a manner similar to the well-known quinolone drugs. Quinolones 178-187 DNA topoisomerase II alpha Homo sapiens 37-47 11089230-0 2001 Quinolone interactions with DNA and DNA gyrase. Quinolones 0-9 DNA topoisomerase II alpha Homo sapiens 36-46 11178337-1 2001 The therapeutic use of DNA gyrase inhibitors, mainly quinolone antibacterials, has proven to be a tremendous success story in the treatment of bacterial infections. Quinolones 53-62 DNA topoisomerase II alpha Homo sapiens 23-33 11408214-1 2001 DNA gyrase is a target of quinolone antibacterial agents, but the molecular details of the quinolone-gyrase interaction are not clear. Quinolones 26-35 DNA topoisomerase II alpha Homo sapiens 0-10 11408214-1 2001 DNA gyrase is a target of quinolone antibacterial agents, but the molecular details of the quinolone-gyrase interaction are not clear. Quinolones 91-100 DNA topoisomerase II alpha Homo sapiens 0-10 11399091-0 2001 gyrB-225, a mutation of DNA gyrase that compensates for topoisomerase I deficiency: investigation of its low activity and quinolone hypersensitivity. Quinolones 122-131 DNA topoisomerase II alpha Homo sapiens 24-34 9207016-0 1997 DNA gyrase can cleave short DNA fragments in the presence of quinolone drugs. Quinolones 61-70 DNA topoisomerase II alpha Homo sapiens 0-10 11249592-2 2000 Hokuriku is developing olamufloxacin, a quinolone antibiotic that inhibits DNA gyrase, for the potential treatment of various types of bacterial infection. Quinolones 40-49 DNA topoisomerase II alpha Homo sapiens 75-85 11097055-0 2000 The interaction of drugs with DNA gyrase: a model for the molecular basis of quinolone action. Quinolones 77-86 DNA topoisomerase II alpha Homo sapiens 30-40 11097062-1 2000 A new 6-desfluoroquinolone derivative, characterized by the presence of a 6-hydroxyl group instead of the usual fluorine atom at the C-6 position, was synthesized with the aim to better understand the mechanistic role of the C-6 substituent in the quinolone/DNA/DNA-gyrase interaction. Quinolones 17-26 DNA topoisomerase II alpha Homo sapiens 262-272 10377219-1 1999 The bacterial topoisomerase II (DNA gyrase) and the mammalian topoisomerase II represent the cellular targets for quinolone antibacterials and a wide variety of anticancer drugs, respectively. Quinolones 114-123 DNA topoisomerase II alpha Homo sapiens 32-42 9717215-1 1998 DNA gyrase is an essential topoisomerase that is found in all bacteria and is the target of potent antibiotics, such as the quinolones. Quinolones 124-134 DNA topoisomerase II alpha Homo sapiens 0-10 9379449-6 1997 Molecular modeling of 4a indicates that the diphenic acid monohydroxamides can bind to the DNA-DNA gyrase complex in a similar fashion as that hypothesized for the quinolone series according to the hypothesis suggested by Shen et al. Quinolones 164-173 DNA topoisomerase II alpha Homo sapiens 95-105 11053451-0 2000 DNA gyrase-mediated wrapping of the DNA strand is required for the replication fork arrest by the DNA gyrase-quinolone-DNA ternary complex. Quinolones 109-118 DNA topoisomerase II alpha Homo sapiens 0-10 11053451-0 2000 DNA gyrase-mediated wrapping of the DNA strand is required for the replication fork arrest by the DNA gyrase-quinolone-DNA ternary complex. Quinolones 109-118 DNA topoisomerase II alpha Homo sapiens 98-108 9748648-6 1998 Finally, analysis of drug-resistance mutations in the T4 topoisomerase have implicated certain regions of the protein in drug interaction and provided a strong link between the mechanism of action of the antibacterial quinolones, which inhibit DNA gyrase, and the various antitumor agents, which inhibit mammalian type II topoisomerase. Quinolones 218-228 DNA topoisomerase II alpha Homo sapiens 244-254 9712890-0 1998 The DNA gyrase-quinolone complex. Quinolones 15-24 DNA topoisomerase II alpha Homo sapiens 4-14 9712890-12 1998 We demonstrate that quinolone binding and drug-induced DNA cleavage are separate processes constituting two sequential steps in the mechanism of action of quinolones on DNA gyrase. Quinolones 20-29 DNA topoisomerase II alpha Homo sapiens 169-179 9712890-12 1998 We demonstrate that quinolone binding and drug-induced DNA cleavage are separate processes constituting two sequential steps in the mechanism of action of quinolones on DNA gyrase. Quinolones 155-165 DNA topoisomerase II alpha Homo sapiens 169-179 9703246-5 1998 Furthermore, oxolinic acid was found to enhance DNA binding of the gyrase having GyrB (acrB-K447E), supporting a recent proposal that quinolone binding to the DNA-gyrase complex does not require DNA breakage. Quinolones 134-143 DNA topoisomerase II alpha Homo sapiens 159-169 7875053-3 1994 Quinolone antibacterial agents have been shown to be inhibitors of DNA gyrase, a bacterial topoisomerase II enzyme. Quinolones 0-9 DNA topoisomerase II alpha Homo sapiens 67-77 8843280-11 1996 The binding potencies of the two enantiomers and two other quinolones correlated well with their respective concentrations causing 50% inhibition against DNA gyrase. Quinolones 59-69 DNA topoisomerase II alpha Homo sapiens 154-164 8843280-16 1996 This greater number of molecules optimizes the interaction between the drug and the enzyme, possibly through a contact between the C-7 substituent and the quinolone pocket on the B subunit of DNA gyrase. Quinolones 155-164 DNA topoisomerase II alpha Homo sapiens 192-202 7695300-0 1995 Effect of pyrimido[1,6-a]benzimidazoles, quinolones, and Ca2+ on the DNA gyrase-mediated cleavage reaction. Quinolones 41-51 DNA topoisomerase II alpha Homo sapiens 69-79 7695300-1 1995 The quinolones inhibit the A subunit of DNA gyrase in the presence of Mg2+ by interrupting the DNA breakage and resealing steps, and the latter step is also retarded without quinolones if Mg2+ is replaced by Ca2+. Quinolones 4-14 DNA topoisomerase II alpha Homo sapiens 40-50 7695300-1 1995 The quinolones inhibit the A subunit of DNA gyrase in the presence of Mg2+ by interrupting the DNA breakage and resealing steps, and the latter step is also retarded without quinolones if Mg2+ is replaced by Ca2+. Quinolones 174-184 DNA topoisomerase II alpha Homo sapiens 40-50 7695300-4 1995 Each contained, at a different position, the 20-bp pBR322 sequence around position 990, where DNA gyrase preferentially cleaves in the presence of quinolones. Quinolones 147-157 DNA topoisomerase II alpha Homo sapiens 94-104 7695300-5 1995 Our results show that pyrimido[1,6-a]benzimidazoles have a mode of action similar to that of quinolones; they inhibit the resealing step and influence the DNA sequence specificity of DNA gyrase in the same way. Quinolones 93-103 DNA topoisomerase II alpha Homo sapiens 183-193 7868402-10 1994 Alternatively, reduced activity may be due to a fundamental effect on the interaction between quinolones and their target DNA gyrase. Quinolones 94-104 DNA topoisomerase II alpha Homo sapiens 122-132 7853333-7 1995 Based upon the proposed model for the 2:2 quinobenzoxazine:Mg2+ complex on DNA, a parallel model for the antibacterial quinolone-Mg2(+)-DNA gyrase complex is proposed that relies upon the ATP-fueled unwinding of DNA by gyrase downstream of the cleavable complex site. Quinolones 119-128 DNA topoisomerase II alpha Homo sapiens 136-146 7826863-0 1994 Molecular mechanisms of DNA gyrase inhibition by quinolone antibacterials. Quinolones 49-58 DNA topoisomerase II alpha Homo sapiens 24-34 8137121-1 1993 Antibacterial quinolones are thought to inhibit DNA gyrase by trapping the enzyme as a complex with the DNA substrate. Quinolones 14-24 DNA topoisomerase II alpha Homo sapiens 48-58 1319080-0 1992 Mode of action of new quinolones: the inhibitory activity on DNA gyrase. Quinolones 22-32 DNA topoisomerase II alpha Homo sapiens 61-71 1338309-2 1992 Quinolone antibacterial agents have been shown to be inhibitors of DNA gyrase, a bacterial topoisomerase II enzyme. Quinolones 0-9 DNA topoisomerase II alpha Homo sapiens 67-77 2162298-1 1990 Bacterial resistance to quinolones is essentially the result of mutations on several genes involved in the synthesis of DNA-gyrase or in proteins of the cellular envelope. Quinolones 24-34 DNA topoisomerase II alpha Homo sapiens 120-130 1850968-1 1991 A study was made of the correlation between the in vitro inhibitory effects of several quinolones, including four ofloxacin derivatives, on bacterial DNA gyrase from Escherichia coli KL-16 and on topoisomerase II from fetal calf thymus. Quinolones 87-97 DNA topoisomerase II alpha Homo sapiens 150-160