The DNA Gyrase-Quinolone Complex: ATP HYDROLYSIS AND THE MECHANISM OF DNA CLEAVAGE *
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It is demonstrated 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, which is capable of ATP hydrolysis through an alternative pathway involving two different conformations of the enzyme.About:
This article is published in Journal of Biological Chemistry.The article was published on 1998-08-28 and is currently open access. It has received 111 citations till now. The article focuses on the topics: DNA gyrase & DNA supercoil.read more
Citations
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Clinical Pharmacokinetics, Safety and Exploratory Efficacy Study of a Topical Bactericidal VB-1953: Analysis of Single and Multiple Doses in a Phase I Trial in Acne Vulgaris Subjects
TL;DR: VB-1953 topical gel appears to be safe for use in adults with facial acne vulgaris and may offer new advances as a topical antibiotic agent for the disease.
Book ChapterDOI
DNA-Synthesizing Enzymes as Antibacterial Targets
Carlos Barreiro,Ricardo V. Ullán +1 more
TL;DR: These enzymes, which present characteristics that differentiate the replisome of bacteria from that of virus, archaea or eukaryotes, have been extensively studied in the last decades as antibacterial targets with divergence in outcomes as stated in this chapter.
Journal ArticleDOI
Synthesis, characterization, antibacterial activities testing and the interaction of DNA with ciprofloxacin and its La(III)-based complex
TL;DR: La(III) complex, [LaIII(H2O)4(L)2]Cl (2) {L = ciprofloxacin (1)}, was synthesized and characterized by elemental analysis, Infra-red (IR), Ultra-violet (UV) visible spectra, Nuclear magnetic resone...
Posted ContentDOI
Quantitatively predicting optimal antibiotic dose levels from drug-target binding
Fabrizio Clarelli,Adam C. Palmer,Bhupender Singh,Merete Storflor,Silje Lauksund,Ted Cohen,Sören Abel,Sören Abel,Pia Abel zur Wiesch,Pia Abel zur Wiesch +9 more
TL;DR: A computational model (COMBAT-COmputational Model of Bacterial Antibiotic Target-binding) that leverages accessible biochemical parameters to quantitatively predict the antimicrobial effects of antibiotics based on their drug-target affinity is described.
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Mechanisms of antibiotic action shape the fitness landscapes of resistance mutations
Pia Abel zur Wiesch,Colin Hemez +1 more
TL;DR: In this paper , a model that links bacterial population dynamics with antibiotic-target binding kinetics was developed to derive mechanistic insights on drug activity from population-scale experimental data and quantify the interplay between drug mechanism and resistance selection.
References
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Theoretical aspects of DNA-protein interactions: co-operative and non-co-operative binding of large ligands to a one-dimensional homogeneous lattice.
TL;DR: The results indicate that the binding of any non-interacting ligand covering more than one lattice residue results in non- linear (convex downward) Scatchard plots, and the introduction of positive ligand-ligand co-operativity antagonizes this non-linearity, and eventually leads to plots of the opposite curvature.
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Nalidixic acid resistance: A second genetic character involved in DNA gyrase activity
TL;DR: The nalA locus is responsible for a second component needed for DNA gyrase activity in addition to the component determined by the previously described locus for resistance to novobiocin and coumermycin (cou), which appears to be involved in the nicking-closing activity required in the supercoiling reaction.
Journal ArticleDOI
Crystal structure of the breakage-reunion domain of DNA gyrase
Joo H. Morais Cabral,Andrew P. Jackson,Clare V. Smith,Nita Shikotra,Anthony Maxwell,Robert C. Liddington +5 more
TL;DR: The crystal structure of the breakage-reunion domain of DNA gyrase at 2.8 A resolution was presented in this paper, where it was shown that the two structures represent two principal conformations that participate in the enzymatic pathway.
Journal ArticleDOI
Mechanism of inhibition of DNA gyrase by quinolone antibacterials: a cooperative drug--DNA binding model.
Linus L. Shen,Lester A. Mitscher,Padam N. Sharma,T. J. O'Donnell,Daniel W. T. Chu,Curt S. Cooper,Terry J. Rosen,Andre G. Pernet +7 more
TL;DR: A cooperative quinolone-DNA binding model for the inhibition of DNA gyrase and the unique self-association phenomenon (from which the cooperativity is derived) of the drug molecules to fit the binding pocket with a high degree of flexibility is proposed.
Journal ArticleDOI
Energy coupling in DNA gyrase and the mechanism of action of novobiocin
TL;DR: It is postulate that ATP and App[NH]p are allosteric effectors of a conformational change of gyrase that leads to one round of supercoiling and that cyclic conformational changes accompanying alteration in nucleotide affinity also seem to be a common feature of energy transduction in other diverse processes including muscle contraction, protein synthesis, and oxidative phosphorylation.