Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 29 for “"Gyrase"”.
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Staphylococcus aureus DNA gyrase: mechanism and drug targeting
… the development of antibiotic resistance. DNA gyrase is an essential bacterial type II DNA topoisomerase that manipulates DNA topology by performing transient double-strand breaks and DNA strand passage. As gyrase is vital for bacterial survival, it is an effective antibacterial target. By …
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Molecular modelling assisted design and synthesis of cyclothialidine derivatives as DNA gyrase inhibitors
… was discovered as the most active DNA gyrase inhibitor in 1994, enormous efforts have been devoted to make it into a commercial medicine by a number of pharmaceutical companies and research groups worldwide. However, no serious breakthrough has been made up to now. An essential problem …
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Phytochemical and biological investigation of erigeron annus (L.) Pers for antimicrobial activity and potential DNA gyrase inhibitors
… composition, antibacterial activity, DNA gyrase inhibitory activity and mutagenicity assessment were evaluated on isolated compounds and extracts.
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Investigations of Novel Mechanisms of Action for Anti-Bacterial and Anti-Cancer Agent Development
… is an angucyclinone antibiotic that inhibits DNA gyrase with a novel mechanism of action that has been termed competitive inhibition. Simocyclinone D8 was found to inhibit the growth of both Gram-(+ve) and Gram-(–ve) organisms and also inhibit a fluoroquinolone resistant mutant of DNA gyrase. …
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A fragment based approach to the development of novel antibacterial agents inspired by the natural product simocyclinone D8
… mechanism of simocyclinone D8 (SD8) against DNA gyrase has inspired medicinal chemists for over a decade. The search for antibiotics with new mechanisms of action has never been more important with ever increasing prevalence of resistance. This project had three objectives. Firstly to contribute …
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Towards the total synthesis of novenamine and its analogues with modifications at C-4 and C-5
… unit. Its activity as a DNA-gyrase inhibitor and the absence of analogues containing 4-epi-noviose provided the rationale for developing new synthetic routes to these analogues. This thesis describes the total synthesis of the methyl glycosides of noviose and C-4-epi-noviose, …
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In silico-guided design, synthesis and antimicrobial activity of piperazine-linked 8-hydroxyquinoline-isatin hybrids
… coli’s outer membrane protein A (OmpA) and DNA gyrase as the key target enzymes. Both 14c and 15c showed binding energies of -9.8 kcal/mol with OmpA. In the case of DNA gyrase, a binding energy of -8.9 kcal/mol was recorded for 14c, whereas 15c showed satisfactory interaction with a binding …
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Transposable prophage Mu exists as an independent chromosomal domain in E. coli
… of the Mu 'domain' configuration are a strong gyrase site SGS at the center of Mu, the Mu L end, the MuB protein, and the E. coli nucleoid-associated proteins IHF, Fis and HU. The Mu domain was observed at two structurally different chromosomal locations, and was specific to the Mu prophage, …
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A role for the Bacillus subtilis Structural Maintenance of Chromosomes (BsSMC) protein in chromosome organization and compaction
… mutant is hypersensitive to inhibitors of DNA gyrase, which reduce the level of negative supercoiling in the cell. Conversely, depletion of Topoisomerase I, which increases the amount of negative supercoiling of the chromosome, partially suppresses the phenotype of an smc null mutant. These …
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Nutzung und Komplikationen getunnelter zentralvenöser Hämodialysekatheter
… and 2003, to cepholosporins from 17% to 38%, to gyrase inhibitors from 23% to 41% and to aminoglycosides from 22% to 35%. Major complications of tunneled, cuffed central venous catheters are thrombosis and infection with a increase in resistance of causitive pathogens. Nevertheless, these …
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Super-Resolved Microscopy as a Tool to Unveil Intracellular Structure in Biological Systems
… of the bacterial chromosome. By inhibiting DNA gyrase in exponential phase, we were able to observe a very similar reorganization of H-NS, and chromosomal collapse, that we previously observed only in stationary phase. This behavior implies that the superhelicity of the chromosome plays a role …
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DNA supercoiling with a twist
… antibiotic which otherwise targets DNA gyrase and topoisomerase IV. Enrofloxacin inhibits DNA relaxation by Vaccinia topoisomerase I. When presented with relaxed DNA, the enzyme executes the reverse reaction, supercoiling the DNA. Enrofloxacin does not interfere with the catalytic …
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Understanding the Genetics and Evolution of Antimicrobial Resistance in Escherichia Coli
… of 30 genes whose knockdown reduced the level of gyrase-mediated quinolone resistance inE. coli. Finally, to gain understanding of the network of genes contributing to intrinsic and phenotypic resistance, I have studiedE. coli's two-component signal transduction systems (TCS). TCSs are involved in …
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Algorithmic Developments for Sequence Analysis, Structure Modeling and Functional Prediction of Proteins
… First, the structure of C-terminal domain of Gyrase A is predicted through inferred homology relationship with regulator of chromosome condensation (RCC1). This prediction has been validated by experimental data. Second, a hierarchical structure classification of thioredoxin-like fold proteins …
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Mathematical and experimental approaches to the dimer catastrophe theory
… that may be achievable endogenously. DNA gyrase was investigated as a component of the mechanism of this inhibition, and indole was found to inhibit its supercoiling activity in vitro.
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Water in Protein Cavities: Free Energy, Entropy, Enthalpy, and its Influences on Protein Structure and Flexibility
… antibiotics novobiocin and clorobiocin with DNA gyrase are illustrative of the importance of bound water to binding thermodynamics. Mutants resistantto novobiocin as well as those with a decreased affinity for novobiocin over clorobiocinboth involve a less favorable entropy of binding, which more …
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