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.
Results
Showing 1 to 20 of 20 for “"DNA gyrase"”.
-
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 …
-
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 …
-
Phytochemical and biological investigation of erigeron annus (L.) Pers for antimicrobial activity and potential DNA gyrase inhibitors
… chemical composition, antibacterial activity, DNA gyrase inhibitory activity and mutagenicity assessment were evaluated on isolated compounds and extracts.
-
Investigations of Novel Mechanisms of Action for Anti-Bacterial and Anti-Cancer Agent Development
… D8 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. …
-
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 …
-
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 …
-
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 …
-
A role for the Bacillus subtilis Structural Maintenance of Chromosomes (BsSMC) protein in chromosome organization and compaction
… must compact their chromosomes in order for the DNA to fit inside the cell or nucleus. In Bacillus subtilis, and other bacteria, replication occurs simultaneously with the organization, compaction and segregation of newly duplicated chromosomal regions. My work indicates that the B. subtilis …
-
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 …
-
DNA supercoiling with a twist
The level of torsion in double-stranded DNA regulates base-pair stability and DNA conformation. It is important in initiation and regulation of specific DNA metabolic processes as well as chromatin assembly. High mobility group proteins (HMGB) are architectural proteins whose HMG DNA binding …
-
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.
-
Water in Protein Cavities: Free Energy, Entropy, Enthalpy, and its Influences on Protein Structure and Flexibility
… the 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 …
-
Molecular Characterization of Fluoroquinolone Resistance in Streptococcus pneumoniae
… resistance determining regions (QRDRs) of DNA gyrase and/or DNA topoisomerase IV, and (2) drug efflux via unknown transporter proteins. Although previous studies have examined the selection of these resistance mechanisms to varying degrees, a more rigorous and extensive investigation was …
-
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 …
-
Cargo delivery into gram-negative bacteria via enterobactin uptake machinery
… are widely used antibiotics that target DNA gyrase. Prior studies with siderophore-fluoroquinolone conjugates suggest that a release step is required following cytosolic entry for the conjugates to exhibit antimicrobial activity. We design and synthesize enterobactin-fluoroquinolone …
-
Antibiotic Tolerance and Heteroresistance: Associated Fitness Costs and Potential in Evading Antibiotic Killing
… on-target mutations in topoisomerase IV parC and DNA gyrase gyrA. The wild-type S. pneumoniae TIGR4 was not readily transformed with single mutations in gyrA or parC; however, it was readily transformed with double on-target mutations in gyrA and parC. Compared to the wild type, the single …
-
Deoxynyboquinones as NQO1-targeted anticancer compounds and deoxynybomycins as potent and selective antibiotics
Made available in DSpace on 2016-03-02T20:57:24Z (GMT). No. of bitstreams: 5 PARKINSON-DISSERTATION-2015.pdf: 21604741 bytes, checksum: 36ce90169c82a68c9b09739d5545d439 (MD5) LICENSE.txt: 4216 bytes, checksum: 30a9874759f4e96d3a10d148120d7757 (MD5) Parkinson Supplemental 1.pdf: 124148 bytes, …