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 23 for “"Taxanes"”.
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Targeting LEDGF/p75 to Sensitize Chemoresistant Prostate Cancer Cells to Taxanes
… (DTX). These cells also showed resistance to the taxanes cabazitaxel (CBZ) and paclitaxel (PTX), but not to the classical inducer of apoptosis TRAIL. Silencing LEDGF/p75 effectively sensitized taxane-resistant PC3 and DU145 cells to DTX and CBZ, as evidenced by a significant decrease in their …
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Development of novel extraction and separation methods for the determination of anthracyclines and taxanes simultaneously from biological matrices
… the fact that a mixture of anthracyclines and taxanes may be administered simultaneously to patients and that accurate measurement of drug levels during chemotherapy is proven to be more beneficial to patients, currently no chromatographic method exists for the measurement of any anthracycline …
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EFFECT OF MICROTUBULE-TARGETING AGENTS ON STRUCTURAL SIGNALING AND CHEMICAL TRANSPORT IN CELLS
… depolymerization events. Although the ability of taxanes to disrupt microtubule dynamics is closely linked to their chemotherapeutic effects, the exact cellular mechanism behind their anticancer activity remains under debate. At present, taxanes remain among the first-line treatments for several …
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Targeting PRMT5 impairs cancer proliferation through splicing but promotes state shifts that enable resistance and disease progression
… relevance, as co-treatment with PRMT5i and taxanes was highly effective at killing multiple cancer cell lines, and suppressed the emergence of PRMT5i resistance. Moreover, analysis of patient data showed that STMN2 levels serve as a biomarker to predict patient response to taxanes. We also …
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Further investigation of capillary electrophoresis for pharmaceutical analysis
… types of anticancer drugs - anthracyclines and taxanes. The high hydrophobicity of the drugs requires detailed investigation of suitable buffer composition with additives of miscellaneous component and organic phase. The use of these drugs in combination therapy sparked the interest in this …
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Determining the mechanism of double-stranded RNA-induced cell death in ovarian cancer.
… Current ovarian cancer drug regimens, including taxanes and platinum-based agents, are susceptible to chemoresistance necessitating the development of novel chemotherapeutics. Within tumors pathogen-derived ligands, such as dsRNA, can activate pattern recognition receptors (PRRs) that are capable …
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The Status of the Genus Taxus In Kentucky
… differences between taxa utilizing only five taxanes. GIS models were prepared for 13 counties in eastern Kentucky, and these predicted the most likely occurrence of Taxus canadensis in each portion of the county. This study documented three species of Taxus that occur in Kentucky, T. baccata, …
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Docetaxel uptake and modulation of P-gpmediated docetaxel efflux by tyrosine kinase inhibitors in human lung carcinoma cell lines
Treatment with the taxanes, docetaxel and paclitaxel, can result in the emergence of multi-drug resistance (MDR) mediated by P-gp (MDR-1, ABCB1), which is an effective cellular efflux pump for both agents. This thesis was undertaken to examine the contribution of drug transport mechanisms to …
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The Therapeutic Targeting Of Folate Receptor Alpha Positive Tumors Via Folate Receptor Selective Novel 5- And 6- Substituted Pyrrolo [2,3-D]pyrimidine Antifolates"
… when the use of platinum-based therapies and taxanes were introduced.</p> <p>Approximately 90 percent of EOC are folate receptor alpha (FRα) positive with the extent of receptor over-expression corresponding with stage and grade of disease. FRα based therapies are a subject of increasing …
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Chemoligand therapy for metastatic castration-resistant prostate cancer
… for radioligand therapy. After screening taxanes, auristatins, and maytansinoids as candidates for drug development, I conjugated the next-generation microtubule inhibitor monomethyl auristatin E into glutamate-ureido-based small molecules via a multimodality chelator pioneered in our …
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Platelets and Anti-Angiogenic Resistance In Ovarian Carcinoma
… suggested minimal platelet sequestration of taxanes. Blockade of platelet activation blocked <em>in vitro</em> effects. <em>In vivo</em>, thrombocytosis blocked chemotherapeutic efficacy, thrombocytopenia increased chemotherapeutic efficacy, and aspirin therapy partially blocked the effects …
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Design and synthesis of pyrimido[4,5-b]indoles and furo[2,3-d]pyrimidines as single agents with combination chemotherapy potential or as inhibitors of tubulin or thymidylate synthase
… 4-anilino-5-methyl-furo[2,3-d]pyrimidines.</p><p> Taxanes and vinca alkaloids are widely used tubulin inhibitors in cancer chemotherapy. However, their clinical use is compromised by two major mechanisms of drug resistance: the overexpression of Pgp and bIII-tubulin. This dissertation describes the …
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Neurochemical characterization of primary sensory neurons in a rat model of bortezomic-induced peripheral neuropathy
… agents, including platinum drugs, taxanes, epothilones and vinca alkaloids, but also newer agents such as bortezomib. Bortezomib (VELCADE) is a boronic acid dipeptide, which causes a selective blockade of proteasome activity. Bortezomib-induced peripheral neuropathy is an important …
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C—H oxidation reactions: development and application
… catalyst is used to explore oxidations of taxanes, the core structure found in the anti-cancer agent paclitaxel. Hydrogen-abstraction/ring contraction suggested a new late-stage, P450-mediated biosynthetic hypothesis for the formation of A-ring nortaxane natural products, and demonstrated …
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Novel combination strategies with Aurora Kinase Inhibitors: using pre-clinical data to guide clinical trial design
… efficacy of AK-A inhibitors in combination with taxanes but at the expense of additive toxicity. My work suggests that using AK-A inhibitors with lower concentrations of paclitaxel could reduce toxicity, highlighting the need to explore a range of combinations. Existing early phase clinical data …
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An innate immune response to DNA damage in prostate cancer
… to assess response platinum, PARP inhibitors and taxanes. Subsequently a siRNA mediated screen was completed to try and identify novel gene mutations, which may contribute to BRCAness phenotype. Formalin-fixed, paraffin- embedded (FFPE) diagnostic core biopsies were obtained from 52 men with …
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Identification of novel determinants of primary and acquired resistance to EGFR-targeted therapies in colorectal cancer
… demonstrated that combination of ONC201 and taxanes mediated an synergistic apoptotic effect, which was initially demonstrated in BRAFMT cell lines. This treatment strategy was also shown to display efficacy within LIM1215 CRC cells with an acquired KRAS mutation. This chapter therefore …
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Target Based Design And Synthesis of Heterocycles in the Potential Treatment of Cancer and Opportunistic Infection
… the failure of clinically used agents such as taxanes and vinca alkaloids. A series of monocyclic pyrimidine analogs were designed and synthesized as colchicine site binding agents to overcome Pgp and β-III tubulin meditaed drug resistance.<br /> Multitargeted single agents with dual mechanism …
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Catalytic promiscuity of two plant P450 enzymes: CYP725A4 from Taxus cuspidata and CYP71B102 from Isatis Tinctoria
… trace amounts of unidentified monooxygenated taxanes. The presence of T5α-ol was confirmed by comparing its gas chromatography and mass spectroscopy (GC-MS) retention time and spectrum with a standard T5α-ol, while those of others were verified by matching mass spectra from previous studies. …
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Discovery of Inhibitors of Inhibitors of Apoptosis Proteins and Novel Tubulin Polymerization Inhibitors as Potential Anticancer Agents
… death. Unlike the clinically used antitubulins, taxanes and vinca alkaloids, CBSIs are less prone to several known clinical taxanes resistance mechanisms and possess improved aqueous solubility. Our lab previously reported the discovery of VERU-111, a potent and orally bioavailable CBSI with …
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