Mechanism of inhibition of DNA gyrase by cyclothialidine, a novel DNA gyrase inhibitor

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Cyclothialidine analogs, novel DNA gyrase inhibitors.

DNA gyrase inhibitors, cyclothialidines B, C, D and E were isolated from four Streptomycete strains (NR 0659, NR 0660, NR 0661 and NR 0662). Their structures have been elucidated based on the amino acid analysis of the hydrolysates, NMR and HRFAB-MS experiments and shown to be cyclothialidine analogs. The absolute stereochemistry has been determined by the chiral HPLC analysis of the hydrolysat...

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Cyclothialidine, a novel DNA gyrase inhibitor. I. Screening, taxonomy, fermentation and biological activity.

Streptomyces filipinensis NR 0484 produced a new DNA gyrase inhibitor, cyclothialidine. It showed potent activity against DNA gyrases from Escherichia coli and Micrococcus luteus.

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The phytotoxin albicidin is a novel inhibitor of DNA gyrase.

Xanthomonas albilineans produces a family of polyketide-peptide compounds called albicidins which are highly potent antibiotics and phytotoxins as a result of their inhibition of prokaryotic DNA replication. Here we show that albicidin is a potent inhibitor of the supercoiling activity of bacterial and plant DNA gyrases, with 50% inhibitory concentrations (40 to 50 nM) less than those of most c...

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Mechanism of action of DNA gyrase

DNA gyrase is a bacterial motor protein in a class known as topoisomerases, which are responsible for controlling the topological properties of DNA (e.g. amount of supercoiling or catenation). Most topoisomerases can relax supercoiled DNA, which is an energetically favourable process. DNA gyrase is unique amongst this class, because it can introduce supercoils as well as remove them. To wind or...

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The Naphthoquinone Diospyrin Is an Inhibitor of DNA Gyrase with a Novel Mechanism of Action*

Tuberculosis and other bacterial diseases represent a significant threat to human health. The DNA topoisomerases are excellent targets for chemotherapy, and DNA gyrase in particular is a well-validated target for antibacterial agents. Naphthoquinones (e.g. diospyrin and 7-methyljuglone) have been shown to have therapeutic potential, particularly against Mycobacterium tuberculosis. We have found...

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ژورنال

عنوان ژورنال: Antimicrobial Agents and Chemotherapy

سال: 1994

ISSN: 0066-4804,1098-6596

DOI: 10.1128/aac.38.9.1966