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Advances in DNA gyrase inhibitors

Expert Opinion on Investigational Drugs, 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. The rapid changes in quinolone research and development in recent years have produced several new quinolones: moxifloxacin, gatifloxacin, gemifloxacin and des-6-fluoroquinolone ...
O K, Kim, K, Ohemeng, J F, Barrett
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Targeting DNA gyrase

Expert Opinion on Therapeutic Targets, 2001
The discovery of the peptide DNA gyrase inhibitor microcin B17 (MccB17) in the early 1990s provided a new tool and hope for a novel peptide-based chemical starting point for a new generation of DNA gyrase inhibitors but the definitive mechanism-of-action of MccB17 has remained unknown.
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Formation and resolution of DNA catenanes by DNA gyrase

Cell, 1980
We have discovered that DNA gyrase interlocks duplex DNA circles to form catenanes and resolves catenanes into component monomers. The reactions were inhibited by novobiocin and oxolinic acid and required ATP, Mg++ and spermidine. DNA sequence homology is not involved in catenation, since hybrid catenanes were formed efficiently between supercoiled phi
K N, Kreuzer, N R, Cozzarelli
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Escherichia coli DNA Gyrase

1984
The role of DNA gyrase -a type II topoisomerase- had been speculated about for a long time before the discovery of the enzyme. In 1963, J. Cairns (1) pointed out that the Escherichia coli chromosome is a closed circular double strand DNA molecule. It has consequently become apparent that a replication machinery which has to unwind the two strands would
E, Orr, H, Lother, R, Lurz, E, Wahle
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DNA gyrase as a drug target

Trends in Microbiology, 1997
DNA gyrase is a remarkable enzyme, catalysing the seemingly complex reaction of DNA supercoiling. As gyrase is essential in prokaryotes, it is a good target for antibacterial agents. These agents have diverse chemical structures and interact with gyrase in a variety of ways.
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DNA linking potential generated by gyrase

European Journal of Biochemistry, 1990
Whether or not DNA gyrase can supercoil DNA so that alternative structures will arise in it is the major question of this work. We have shown gyrase to produce in pAO3 DNA a superhelix density sufficient for cruciform formation. However, the transition does not take place because of too slow kinetics.
S A, Kozyavkin   +3 more
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Bacterial death by DNA gyrase poisoning

Trends in Microbiology, 1998
DNA gyrase is an essential topoisomerase that is found in all bacteria and is the target of potent antibiotics, such as the quinolones. By creating DNA lesions and inducing the bacterial SOS response, these drugs are not only highly cytotoxic but also mutagenic.
Couturier, Martine   +2 more
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Fluoroquinolone-Gyrase-DNA Cleaved Complexes

2017
The quinolones are potent antibacterials that act by forming complexes with DNA and either gyrase or topoisomerase IV. These ternary complexes, called cleaved complexes because the DNA moiety is broken, block replication, transcription, and bacterial growth.
Gan, Luan, Karl, Drlica
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Involvement of DNA gyrase in bacteriophage T7 DNA replication

Nature, 1977
NOVOBIOCIN and the related antibiotic coumermycin A1 (referred to as coumermycin) inhibit the supercoiling of circular double-stranded DNA catalysed by Escherichia coli DNA gyrase1. They also inhibit the replication of chromosomal DNA in E. coli cells2, and of circular double-stranded DNA in cell-free systems from E. coli3–6. The activity of DNA gyrase
T, Itoh, J I, Tomizawa
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Clinical utility of DNA gyrase inhibitors

Pharmacology & Therapeutics, 1989
Quinolone antibiotics provide potentially important therapy for many infections. These DNA gyrase inhibitors are established as excellent therapy of urinary infections and of diarrheal disease. As reviewed, the compounds have important use in respiratory, skin-structure and bone infections.
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