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Showing 1 to 20 of 242 for “"Linkers"”.
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Mechanically Interlocked Linkers for Dynamic Metal-Organic Frameworks
… previous work towards incorporation of rotaxane linkers into metal-organic frameworks. Chapter 2 describes how a paradigm shift in the development of such systems resulted in a robust rotaxane linker that was used to create a novel material, UWDM-1 (University of Windsor Dynamic Material), which …
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Multifunctional Chemical Cross-linkers for Drug Carriers and Molecular Probes
… works highlight the importance of chemical cross-linkers in the design of multifunctional bioconjugates for a variety of applications.
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The Development of Sulfatase-Cleavable Linkers for Antibody-Drug Conjugates
… of arylsulfates as enzymecleavable ADC linkers. These arylsulfates were designed to be cleaved by lysosomal sulfatases, thus revealing a phenolate, primed for 1,6-elimination of a payload within the target cell (Figure 1A). Initially, a panel of model linkers were synthesised using a …
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Porphyrin Cross-Linkers for Generating Soluble Molecularly Imprinted Polymers from Polyethyleneimine
<p>Molecular recognition is vital to many biochemical processes and is at the heart of promising bio-medically related technologies. Molecular imprinting has a long-standing history as a successful method for mimicking the molecular recognition phenomena exhibited by nature, whereby artificial …
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Design of smart linkers and their applications in controlled-release drug delivery systems
… drug conjugates (SMDC). We have prepared acetal linkers featuring coumarin as fluorophore and a duocarmycin analogue as an example of cytotoxic drug. Markedly, it represents the first example a duocarmycin analogue is protected with an acid cleavable moiety. Kinetic studies were performed on …
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Addition of flexible linkers to GPU-accelerated coarse-grained simulations of protein-protein docking
… the optional capability for modelling flexible linkers between rigid domains of a single protein. We implement additional Monte Carlo mutations to allow for movement of residues within linkers, and for movement of domains connected by a linker with respect to each other. We also add potential …
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Design of Cleavable Monomers and Cross-Linkers for the Synthesis of Degradable Polymer Architectures
… the design of cleavable monomers and cross-linkers for the synthesis of degradable materials with different polymer architectures. The first half of this thesis focuses on the design of new degradable bottlebrush and brush-arm star polymers (BASPs) via ring-opening metathesis polymerization …
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Novel Building Blocks for Molecular Imprinting: Pyridine-Based Binding Monomers and Bio-Renewable Cross-Linkers
… prepolymerisation mixture. Bio-renewable cross-linkers were also synthesised from isomannide, isosorbide and 2,5-bis(hydroxymethyl)furan as a greener and bio-sustainable alternative to ethylene glycol dimethacrylate (EGDMA) in the Molecular Imprinting technology. Herein we will report on the …
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Targeted drug delivery by novel polymer-drug conjugates containing linkers cleavable by disease-associated enzymes
… of the attached drugs. Traditionally, linkers are degraded by acidity or by some ubiquitous intracellular enzymes. We incorporate linkers that are sensitive to a specific extracellular enzyme whose overexpression is co-localized with the diseased tissue. The drug molecules remain …
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Characterization of D-boroala as a novel Broad-spectrum antibacterial agent targeting D-Ala-D-Ala ligase & designer linkers : model reactions and linear free energy relationships in the reactivity and design of solid-phase linkers
… efforts to develop a backbone amide attachment linkers with the appropriate chemical stability for ISPPS i.e. stable to 25% TFA/DCM treatment and cleavable with 5% HBr/TFA. Candidate linkers were then loaded onto aminomythylated polystyrene resin to demonstrate an effective method for ISPPS …
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MULTIVARIATE FLEXIBLE METAL ORGANIC FRAMEWORKS: THE ROLE OF FUNCTIONALIZED LINKERS, HETEROGENEITY AND DEFECTS IN ADSORPTION PROCESSES
… to the dangling side chains present on the linkers, which interact with mobile guest molecules as well as with themselves and with the framework backbone. The samples were characterized by a variety of techniques: PXRD, FTIR, TGA, DSC, EFTEMEDX, TEM tomography, UV-Vis and PL spectroscopy, …
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Development of Novel Self-Immolative Linkers based on Fragmentation and Cyclisation Reactions for Targeted Therapeutic Applications
La terapia dirigida se ha erigido a lo largo de los últimos años como una de las estrategias más prometedoras para el tratamiento del cáncer. Estos sistemas consisten en una molécula con una alta afinidad y selectividad hacia una diana presente en células cancerosas, conjugada a fármacos …
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The Development of Divinyl-Heteroaryl Linkers for the Synthesis of Stable and Functional Antibody-Drug Conjugates
… set of divinylpyrimidine (DVP) cysteine bridging linkers. Early investigations into divinylpyridine reagents were initially conducted, but disappointingly, were deemed to have insufficient reactivity to enable efficient antibody disulfide rebridging. Alteration of the divinyl-heteroaryl scaffold …
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Pyrrolo[2,3-d]pyrimidine-based π-conjugated fluorophores with 1,2,3-triazole and ethynyl linkers: synthesis and photophysical properties /
… oligoarylenes with ethynyl and 1,2,3-triazole linkers and to evaluate their photophysical properties. Novel chromophores - 2,4-bis(4-aryl-1,2,3-triazol-1-yl)pyrrolo[2,3-d]pyrimidines were prepared by CuAAC reaction. It was demonstrated that in the CuAAC reaction of …
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Dissection of Connective Beta -Strand Linkers and Their Role in Enzymatic Activities of Escherichia Coli Leucyl -Trna Synthetase
Individual glycine residues, when mutated to proline, misaminoacylate tRNALeu in spite of retaining efficient amino acid editing activities. It is possible that these mutant LeuRSs may have impaired the translocation of editing substrates between the aminoacylation and editing active sites. An …
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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
The Development of Vinylheteroarene Linkers for Proteinogenic Cysteine Modification and Studies Towards Applying (+)-Discodermolide as a Novel Payload in Antibody-Drug Conjugates Hikaru Seki Antibody-drug conjugates (ADCs) are an emerging class of anticancer agents which combine the cell-targeting …
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