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 36 for “"high-throughput screening (HTS)"”.
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Assay development for use in drug discovery against Bovine Trichomoniasis
… of this study was to develop new compound screening assays that will make the discovery of new compounds faster and more accurate. The CellTiter-Glo Luminescent Cell Viability Assay, a high throughput screening (HTS) assay from Promega, was found to be as affective at measuring cytotoxicity …
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A General Purpose Programmable Microfluidic Platform for Screening and Optimization of Biological Assays
Screening is a fundamental process in today’s medicine and clinical diagnostics, comprising of several processes ranging from finding new target molecules having the desired therapeutic potential to identifying biomarkers for accurate diagnosis of a spectrum of diseases. Current high throughput …
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High-Throughput Detection of Protein---Protein and Protein---Dna Interactions via Photonic Crystal Biosensors: Applications to Apoptosis Inducing Factor
"High-throughput screening (HTS) has played an integral role in the discovery of lead molecules that eventually are transformed into the therapies of tomorrow. Contributing towards the success of any screening campaign is the target choice, chemical library size and diversity, as well as the …
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Advances in high-throughput screening: better compounds, novel targets, enhanced sensors
High throughput screening (HTS) is the dominant force in modern drug discovery. Through the evaluation of large structure collections, novel drug leads can be rapidly assessed for modulation of medicinally-relevant biological targets. This occurs through the interplay of three intrinsically linked …
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High-throughput detection of protein—protein and protein—DNA interactions via photonic crystal biosensors: applications to apoptosis inducing factor
High-throughput screening (HTS) has played an integral role in the discovery of lead molecules that eventually are transformed into the therapies of tomorrow. Contributing towards the success of any screening campaign is the target choice, chemical library size and diversity, as well as the …
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High-throughput vertebrate total analysis/screening platform
High-throughput screening (HTS) is seen as one of the most promising technologies to facilitate biomedical studies and pharmaceutical discoveries. Although large varieties of in vitro HTS technologies have opened great opportunities, the speed of improvement has been limited by lack of advanced …
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Discovery of benzamides and triarylimidazoles active against Plasmodium falciparum via haemozoin inhibition : high throughput screening, synthesis and structure-activity relationships
… antimalarials with alternate chemotypes. High throughput screening (HTS) can be used to identify novel scaffolds that inhibit β-haematin (βH - synthetic haemozoin) formation and which have favourable P. falciparum activities. In this project, HTS has been carried out on 43,520 small, …
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Toward High-throughput, Quantitative Platforms to Identify the Targets of Small Molecules
… factors. Here, we developed generalizable, high-throughput platforms that can rapidly identify the mechanism(s) of action of small molecules emerging from high-throughput screening (HTS) campaigns. Specifically, this project established a solid phase method to rapidly modify small molecules …
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Inhibition of enzymes from mycobacteria using fragment-based approaches
… abscessus (Mab). With Mtb fumarase a high-throughput screening (HTS) hit was used to design a small library of fragments in a deconstruction-reconstruction approach. These fragments were screened using a range of both biochemical and biophysical methods. The resultant fragments showed …
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Development of screening assays to test novel integrin antagonists in allergic inflammation
… research: to develop a prototype of homogeneous high-throughput screening (HTS) for identification of novel integrin antagonists for the treatment of ocular allergy and to better understand the mechanisms of action of integrin-mediated levocabastine antiallergic action. Results: This thesis …
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Differential Pax5 Levels Promote Mcl Dispersal and Progression and Predict A Poor Prognosis In Advanced Mcl Patients
… dispersal and progression. We also conducted a high throughput screening (HTS) of 3800 compounds to discover compounds that selectively target the aggressive MCL. The data revealed important properties of PAX5<strong><sup>–</sup></strong> MCL cells, which are highly drug resistant compared to …
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DEVELOPMENT AND KINETIC MODELING OF MULTIPLEX MICROSPHERE ASSAYS FOR HIGH-THROUGHPUT DISCOVERY OF PROTEASE ACTIVE SMALL MOLECULE COMPOUNDS
… simultaneously. In addition, we have performed high-throughput screening (HTS) to identify potential inhibitors for the Bacillus anthracis lethal factor protease (LF) and the Botulinum neurotoxin type A & F light chain proteases (BoNT/A & F LC). In order to select the efficient inhibitors, a …
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Experimental and computational methods for identification of novel fungal histone acetyltransferase Rtt109 inhibitors
… potential drug scaffolds, we employed in vitro high throughput screening (HTS) and various computer-assisted strategies, including molecular dynamics, docking, three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis, pharmacophore modeling, and Support Vector Machine …
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DEVELOPMENT OF A MICROSCALE ELECTROCHEMICAL PLATFORM FOR THE ANALYSIS OF THERMAL PROFILES OF IMMOBILIZED DNA SECONDARY STRUCTURES
… the stability of the structure, leading to higher measured melting temperatures. Development of an electronic platform that can measure the thermal profiles of small-volume samples with automation and methodology that is scalable for high-throughput screening (HTS) would represent an …
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To Design and Develop Semi-Saturated and Unsaturated Bicyclic Heterocycles for Fragment-Based Drug Discovery (FBDD) Campaigns
… seeks to overcome current issues associated with High-Throughput Screening (HTS) for the identification of novel hits, which are ultimately elaborated into leads and drug candidates. This thesis focuses on the preparation of either novel or commercially limited fragments by engaging diverse …
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Toward improved in vitro models for human health risk assessment : mechanisms of short-chain per- and polyfluoroalkyl substances (PFAS) toxicity.
… in response to these issues. While in vitro high-throughput screening (HTS) methods have shown promise, their integration into the existing chemical risk assessment framework faces obstacles concerning physiological relevance. The overarching objective of this dissertation was to enhance our …
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A Fragment-Based Drug Discovery Approach for the Development of Selective Inhibitors of Protein Kinase CK2
… drug discovery (FBDD) has emerged as a highly successful way to provide lead compounds for subsequent optimisation into drug candidates. Initial hits usually exhibit lower potency than those identified by more traditional techniques, such as High-Throughput Screening (HTS), but the …
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Repositioning of astemizole for malaria
… its burden is felt worldwide as seen by the high number of deaths recorded each year (405,000 in 2018: WHO World Malaria Report 2019). Unfortunately, over 90% of this mortality rate is recorded in Africa alone, with the highest risk being in children under the age of five (5) and pregnant …
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Science and technology driving change in drug R&D : some lessons for the Japanese pharmaceutical industry
… methods that use Combinatorial Chemistry (CC), High Throughput Screening (HTS), and Gene Technology. Since the beginning of the 1990s, pharmaceutical companies have actively invested into such technologies. Some investment has been in-house, but many companies have acquired high-tech ventures or …
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Regulation of Cardiomyocyte Proliferation by microRNAs and Small Molecules
… regeneration after cardiac damage. Previous high throughput screening studies in our laboratory identified a series of microRNAs able to trigger cardiomyocyte proliferation and stimulate cardiac regeneration after myocardial infarction. In the first part of this project, we investigated the …
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