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 17 of 17 for “"Pro-drug"”.
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Nitroaromatic pro-drug activation and resistance in the African trypanosome
… sickness. These compounds are believed to act as pro-drugs that require intracellular enzymatic activation for antimicrobial activity. Here, the role of the bacterial-like nitroreductase TbNTR as a nitrodrug activating enzyme is examined through overexpression and knock-out studies in T. brucei. …
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Analogues of Nitrofuran Antibiotics are Potent GroEL/ES Pro-drug Inhibitors with Efficacy against Enterococcus Faecium, Staphylococcus Aureus, and Escherichia Coli
… World Health Organization as some of the most prominent threats to human health, capable of developing significant antibiotic resistance. These pathogens contribute to over 2 million annual infections and ~23,000 annual deaths in the U.S. In addition, various strains of E. coli have also shown …
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Localized and disease-selective drug delivery using adhesive hydrogels for treatment of locally advanced TNBC
… presentation. TNBC is negative for estrogen and progesterone receptor, as well as for HER2, and hence it is not treatable with common endocrine treatment such as tamoxifen or Herceptin. Systemic neoadjuvant therapy has been established as the preferred therapeutic approach for locally advanced …
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Characterization of a transposon-induced pleiotropic metronidazole resistant mutant of Clostridium acetobutylicum P262
Metronidazole is a pro-drug which must be reduced to elicit a bactericidal effect. In the clostridia, some of the electron transport proteins that provide the source of electrons for the reductive activation of metronidazole play a key role in electron distribution, which in turn regulates the …
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Methods for Identifying Subcellular Targeting Ligands and Selected Applications
… plays an essential role in targeting drug therapies as generally the pro-drug or linker relies on physical conditions of a particular subcellular compartment to function. We developed two methods that allow for selecting targeting ligands that both internalize specifically in cancer …
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Sonoptics : applications of light and sound in the context of biomedicine
… of therapeutic agents, which could include drugs and nucleic acids, into biological cells. This process is commonly referred to as 'sonoporation', and the enhanced uptake can be caused through the incident ultrasonic pressure fi eld causing radial oscillations (cavitation) in the …
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Two-Photon Microscopy of E-Combretastatin uptake and activation in live mammalian cells
… are powerful anticancer drugs that are being evaluated in phase I/II clinicaltrials. Combretastatins act by binding to p-tubulin, preventing microtubule assembly andinhibiting angiogenesis in developing tumours. Most widely studied is the natural …
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Synthesis and evaluation of novel antivascular agents for two-photon activation
… Combretastatins are powerful anticancer drugs with some derivatives in advanced clinical trials for cancer therapy. Combretastatins are stilbenes isolated from the African shrub Combretum caffrum. These agents interact with tubulin in a similar way to colchicine, causing destruction of …
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The design and synthesis of novel pro-drugs for the treatment of nephropathic cystinosis.
… number of studies have shown the ability of the drug cysteamine (Cystagon®) to lower cystine accumulation within cells resulting in reduced organ and tissue damage. Cysteamine therapy however, is associated with a number of side effects involving the gastrointestinal tract and the central …
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Reductive metabolism of aliphatic tertiary amine n-oxides.
This study is based on a proposal concerning the feasibility of using aliphatic tertiary amine N-oxides as antiarrhythmic agent prodrugs. Lignocaine was selected as a candidate for prodrug development, because the N-oxide is a non-active, polar derivative of lignocaine and the drug of choice for …
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Viral HSV1-TK gene, radiolabeled FIAU, and ganciclovir: combined gene targeted radiotherapy and suicide gene therapy for prostate cancer
… cells, by gene transfer, to convert a non-toxic pro-drug into a toxic product. Previous work has shown that the combination of herpes simplex virus type 1 thymidine kinase gene (HSV1-tk) transfer with the pro-drug ganciclovir (GCV) to be a promising suicide gene therapy in cancer. Unlike several …
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Drug repurposing against the store-operated calcium entry (SOCE) pathway and subsequent exploration of SOCE in oligodendrocyte progenitor cells
… that regulate a diverse array of biological processes. Abnormal SOCE seem to underlie several diseases that notably include allergy, inflammation, acute pancreatitis and cancer. Therefore, any modulator of this pathway is likely to have significant impact in cell biology under both normal and …
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Investigation of azithromycin analogues and proteasome-like inhibitors as quick-killing antimalarials
… Of current concern is the spread of multi-drug resistant parasites that have severely limited the efficacy of antimalarials, including front-line artemisinins, highlighting the urgent need to identify new antimalarials for use as treatments. The aim of this thesis was to investigate novel …
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Design of smart linkers and their applications in controlled-release drug delivery systems
Antibody drug conjugates (ADC) represents an interesting strategy in tumour targeted therapy . The approach is based on the combination of the high affinity of an antibody towards its antigen and the high cytotoxicity of a drug, leading to a selective therapuetic agent with improved efficacy and …
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Cellular Senescence in Non-Small Cell Lung Cancer: from mechanisms to therapeutic opportunities
… to current treatment paradigms are crucial to improve lung cancer survival. Cellular senescence is a powerful tumour-suppressive mechanism whereby cells stably enter a cell-cycle arrest in response to oncogenic stress. However, the accumulation of senescent cells can alter the tumour …
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The mechanistic basis of susceptibility and resistance to the antitubercular drug para-aminosalicylic acid
… for M. tuberculosis involves lengthy, intensive drug therapy that causes severe side-effects. The antimicrobial para-aminosalicylic acid (PAS) is used to treat drug-resistant M. tuberculosis infections. Despite the use of PAS to treat M. tuberculosis for over 70 years, the biochemical mechanisms …
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Exploring the molecular mechanisms of AMPK-dependent regulation of neuroexcitability
The AMP-activated protein kinase (AMPK) is an energy sensor that maintains cellular metabolic homeostasis in a cell-autonomous manner during energy stress conditions, such as hypoxia and glucose deprivation. Emerging evidence suggests that AMPK activation during metabolic stress conditions may have …