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 26 for “"cytotoxins"”.
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The effects of snake venoms as cytotoxins on selected prostate cancer cell lines
… sequences show homology with the group of cobra cytotoxins/ cardiotoxins from the family Elapidae and are likely to be identical to two known cytotoxins, cardiotoxin γ from N. pallida and cardiotoxin 4 from N. mossambica. Another peptide had an N-terminal sequence similar to a phospholipase A2. …
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An investigation into the metabolic activation of novel chloromethylindolines by isoforms of cytochrome P450. Targeting drug metabolising enzymes in cancer: analysis of the role and function of selected cytochrome P450 oxidising novel cancer prodrugs
… The use of CYPs to activate prodrugs to cytotoxins selectively in tumours has been explored including AQ4N, Phortress and Aminoflavone. CYP1A1, CYP1B1, CYP2W1, and CYP4F11 have been identified as expressed in tumour tissue and surrounding stroma at high frequency compared to most normal …
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The potential of exosome-based gene therapy to eradicate glioblastoma cells
… GBM cells to impair proliferation and the use of cytotoxins to induce apoptosis in the target cells. The plasmids were transfected into exosomes and subsequently inoculated into patient-derived glioblastoma cells with the aim of decreasing the number of glioblastoma cells. The findings of this …
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Development of a Novel Bioconjugation Platform for the Generation of Homogenous Antibody-Drug Conjugates
… of antibodies to selectively deliver potent cytotoxins to specific cell types, such as cancer cells. The pharmacology of an ADC is critically dependent on its stability, homogeneity, and drug-to-antibody ratio (DAR) – all of which are controlled by the chemistry used to attach the drug to the …
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The Development of a Tumour-Responsive Format for Antibody Conjugates
… particular membrane receptors, to deliver potent cytotoxins to a desired cell type. A significant amount of research has been undertaken to improve the performance and pharmacological profile of ADCs, with a predominant focus on the constituents, format, and bioconjugate chemistry—which together …
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Design and synthesis of benzosuberene and tetracyclic-based molecules inspired by natural products as inhibitors of tubulin polymerization and preparation of drug-linker constructs to facilitate tumor selective targeted delivery.
… as both inhibitors of tubulin polymerization and cytotoxins. A subset of these molecules function through a unique dual-mechanism of action as potent cytotoxins and vascular disrupting agents (VDAs)(distinct from other tubulin-binding agents). VDAs result in selective blood flow shutdown to …
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Studies on the effects of sub-minimal inhibitory concentrations of antibiotics on the virulence factors of biofilm bacteria
… from investigation of its secreted proteases and cytotoxins (leucocidin). Virulence-specific azocasein and micro-culture tetrazolium (MTT) assays against both monospecies and binary biofilms of <i>Pseudomonas aeruginosa</i> indicate significant increases in virulence potential of proteases and …
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Metal Mediated Mechanisms of Drug Release
… was applied to the release of prodrugs of the cytotoxins monomethylauristatin E and 5-fluorouracil in cancer cells. A cisplatin-cleavable antibody-drug conjugate was designed and synthesised, and progress towards its biological evaluation will be discussed.
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Subcellular Localization and Activity of the Multidrug Resistance Protein 1
… are traditionally thought to extrude cytotoxins from the cell at the plasma membrane, and they thereby serve as a permeability barrier for drug entry into the cell. Several MDR transporters have been cloned to date, but this study focuses on the functional characterization of one of …
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Development of a post-mitotic, neuronal-astrocytic cell system, for the prediction of acute neurotoxicity in humans
… chemicals (chronic neurotoxin 2,5-hexanedione, cytotoxins 2,3- and 3,4-hexanedione and acute neurotoxins tributyltin- and trimethyltin- chloride) and also provided the non-cytotoxic concentration-range for each compound. Biochemical endpoints examined over the non-cytotoxic range included assays …
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Treponema hyodysenteriae: growth and production of hemolysin
… rather than the rounding effect caused by many cytotoxins.
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Synthesis and biological evaluation of structurally diverse indole-based analogues as inhibitors of tubulin polymerization and synthesis of drug-linker constructs cleavable by enzymes present in the tumor microenvironment.
… demonstrate dual functionality as both potent cytotoxins (antiproliferative agents) and effective vascular disrupting agents (VDAs). Our previous studies led to the discovery of a potent inhibitor of tubulin polymerization and cancer cell growth, OXi8006, and its water-soluble phosphate prodrug …
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A Mutational Analysis of XcpQ, the Outer Membrane Component of the Type II Protein Secretion System From Pseudomonas Aeruginosa
… to secrete a number of hydrolytic enzymes and cytotoxins. Lipase, phospholipase C, alkaline phosphatase, elastase, exotoxin A, LasA protease, and LipC cryptic lipase are exported via a Type II secretion apparatus. XcpQ is the sole outer membrane protein component of this system and is a member …
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The Development of Vinylheteroarene Linkers for Proteinogenic Cysteine Modification and Studies Towards Applying (+)-Discodermolide as a Novel Payload in Antibody-Drug Conjugates
… rapid assembly of ADCs using unexplored alcohol cytotoxins. Using this linker, a discodermolide ADC was successfully synthesised which can be used for biological evaluation.
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Synthesis of a Diverse and Three-Dimensional Fragment Collection and The Development of a Novel Platform for Antibody Dual Functionalisation
… was successfully demonstrated to attach both cytotoxins and fluorophores. Notably, this strategy enabled the generation of theranostic antibody conjugates that exhibited selective in vitro cytotoxicity.
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The Development of Divinyl-Heteroaryl Linkers for the Synthesis of Stable and Functional Antibody-Drug Conjugates
… with biologically-relevant moieties (e.g. cytotoxins, fluorophores) could be achieved either before rebridging with a pre-functionalised linker or after rebridging through bioorthogonal chemistry. In addition, the receptor affinity and cellular selectivity of the antibodies were unaffected …
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Molecular Interactions of Type III Secretion System Transcriptional Regulators in Pseudomonas aeruginosa: ExsA and ExsD
… P. aeruginosa infections by injecting potent cytotoxins (effectors) into host cells to suppress the host's innate immune response. Expression of all T3SS-related genes is strictly dependent upon the transcription factor ExsA. Consequently, ExsA and the biological processes that regulate ExsA …
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Synthesis and bioactivities of novel N¹-acylhydrazides
… = 3.18 µM in MCF-7 cells) were the most potent cytotoxins in series 60. The evaluation of druglike properties revealed that 64a is the lead tumor-specific cytotoxin with an IC50 value of 1.38 µM against HCT 116 cells. When compared against colon CRL-1790 non-malignant cells, these cytotoxic …
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Rational enzyme-directed prodrug development : exploiting tumour hypoxia to target the bioactivation of cytotoxic prodrugs
… have lead to the development of hypoxic-specific cytotoxins. These bioreductive prodrugs rely. on the natural complement of tumour enzymes to catalyse their activation under low tissue oxygen tensions. Levels of these reductases are potentially heterogeneous and are often down-regulated in the …
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