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 8 of 8 for “"Prodrug Activation"”.
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Tetrazine-Triggered Bioorthogonal Decaging Reactions for Prodrug Activation
… for the spatially and temporally controlled activation of proteins and drugs. The inverse electron-demand Diels-Alder (IEDDA) reaction between tetrazines and strained alkenes exhibits high reaction rates and selectivity and has been widely applied for the decaging of amine prodrugs. Although …
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Catalytic antibodies for amide cleavage and prodrug activation
… removing a protection group for the simultaneous activation of multiple prodrugs. To this end, a protective group was designed which could be attached to any kind of cancer drug, in order to convert a cancer drug into a prodrug. The protective group relies on a [beta]-sulfone elimination process …
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T-cell-directed bioorthogonal catalysis for localised prodrug activation in cancer therapy
… but strategies that enable selective activation of therapeutics at the tumour site remain scarce. As a result, there is a continued need for strategies that improve therapeutic efficacy, while minimising systemic toxicities. This thesis investigates the use of bioorthogonal catalysis …
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Tumor-Specific STING Agonist Synthesis via a Two-Component Prodrug System
Pharmacological activation of STING holds promise in cancer treatment. A recent trend is the development of tumor-specific or conditionally activated STING agonists for enhanced safety and efficacy. Herein, we explored an unconventional prodrug activation strategy for on-tumor synthesis of a potent …
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Use of a direct, positive selection strategy to generate improved prodrug-activating enzymes for cancer gene therapy
… currently being studied in combination with the prodrug CB1954, as a gene directed enzyme prodrug therapy. NTR reduces CB1954 at either the 2- or 4-nitro groups to produce highly cytotoxic hydroxylamine derivatives, using either NADH or NADPH as cofactor. Initial clinical trials suggest activity, …
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Designed Bond Cleavage Reactions for Next-Generation Therapeutics
Creating ways for tissue-specific drug activation remains a significant challenge in modern medicine. Traditional approaches to drug delivery often lack precision, leading to unwanted side effects and reduced therapeutic efficacy. This PhD thesis explores two innovative approaches to overcome these …
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Functional Characterization of Serine Hydrolases Mediating Lipid Metabolism and Protein Depalmitoylation in Asexual Stage Plasmodium Falciparum
… Lipases Homolog (XLH) and Plasmodium falciparum prodrug activation and resistance esterase (PfPARE). We generated a series of knockout parasite lines on the AKU-010 targets and identified that red blood cell (RBC)-localized XL2 and cytosolic XLH4 contribute to most LPC hydrolysis activity in the …
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CHEMICAL BIOLOGY STRATEGIES FOR THE FORMATION AND CLEAVAGE OF CHEMICAL BONDS
Chemistry plays an essential role in biological processes within all living organisms and better understanding of how specific chemical bonds can be either formed or broken gives chemical biologists opportunities to control and regulate these processes with high precision. Therefore, with growing …