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 37 for “"compound library"”.
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Synthesis and Structure Activity Relationship Studies of a Natural Product-Derived Compound Library
… been found in this manner, leaving the rarest compounds to still be found. Other drug discovery programs focus on the production of large chemical libraries by combinatorial synthesis. While hundreds of thousands of compounds have been made in this way, only one FDA approved drug has been made …
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Synthesis and Structure Activity Relationship Studies of a Natural Product-Derived Compound Library
… been found in this manner, leaving the rarest compounds to still be found. Other drug discovery programs focus on the production of large chemical libraries by combinatorial synthesis. While hundreds of thousands of compounds have been made in this way, only one FDA approved drug has been made …
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Lead compound discovery for myotonic dystrophy
… for characterization of rationally-designed compounds and the development of a fluorescence anisotropy assay for a high-throughput screening of the NCI Diversity Set III compound library. From such studies I was able to identify several lead compounds that are successful at inhibiting the …
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Gene expression-based screening of inhibitors of signal transduction
… based on the assumption that introduction of a compound into biological system would affect directly or indirectly the gene expression, initiating an elaborate expression response to the disturbance of the system. In my thesis work I investigated new strategies to create a limited expression …
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Targeting The Dimerization Of ERBB Receptor Tyrosine Kinases
… dimerization with small molecules. Two lead compounds were initially predicted by virtual screening the NCI compound library, and were biochemically characterized. The benefit gained from the application of virtual screening in this project initiated another project to enhance the …
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Discovery and Characterization of Novel Chemical Inhibitors of Wnt Ligand Production with Implications for Anti-Cancer Therapy
… this end our laboratory screened a diverse 200K compound library using cell based transcriptional reporters and uncovered several classes of small molecules that modulate distinct Wnt regulatory nodes. One class in particular, termed IWP (Inhibitor of Wnt Production), represents the first …
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Assessment of potential antibacterial drug targets
… kinetic parameters of KynB, Ddl and FolC, and compound library screenings were carried out for Ddl. In parallel, the genetic validation of these targets was being carried out by the Dstl.KynB is an important enzyme in tryptophan metabolism and predicted to be essential in Pseudomonas …
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Targeting RNA With Small Molecules: SL3 of HIV -1 Psi-Rna
… SL3 binders. These studies revealed sixteen compounds with micromolar affinities for RNA, two of which are selective for binding SL3, and another four disrupted NCp7-SL3 interactions. The last chapter describes how a combination of rational structure-based design, molecular modeling, and …
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A NOVEL PIPELINE FOR DRUG DISCOVERY IN NEUROPSYCHIATRIC DISORDERS USING HIGH-CONTENT SINGLE-CELL SCREENING OF SIGNALLING NETWORK RESPONSES EX VIVO
… US Food and Drug Administration (FDA) approved compound library, in addition to experimental neuropsychiatric drug candidates and nutraceuticals, to identify compounds which selectively normalize the schizophrenia-associated cell signalling response. Finally these candidate compounds are …
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Identification of Small Molecule Inhibitors Targeting Truncated Adenomatous Polyposis Coli (APC) as a Novel Therapeutic Strategy in Colorectal Cancer
… cells (HCECs), we have screened a 200K compound library for small molecules that exhibited selective cytotoxicity towards HCECs expressing truncated APC. We identified a compound, TASIN-1(Truncated APC Selective Inhibitor-1), which showed selective cytotoxicity towards HCECs and …
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The use of insect cells to identify potent and selective inhibitors of the replication of the Dengue and Chikungunya viruses and unravel their molecular mechanism of action
… line. In addition we carried out a reference compound library and reference panel of assays and data for DENV, which provides a benchmark for further studies. During this study, a panel of 9 antiviral molecules, with proven in vitro anti-dengue virus activity and that act at different stages …
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Identification of Small Molecule Inhibitors Targeting Truncated Adenomatous Polyposis Coli (APC) as a Novel Therapeutic Strategy in Colorectal Cancer
… cells (HCECs), we have screened a 200K compound library for small molecules that exhibited selective cytotoxicity towards HCECs expressing truncated APC. We identified a compound, TASIN-1(Truncated APC Selective Inhibitor-1), which showed selective cytotoxicity towards HCECs and …
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Mechanisms of action and inhibition of [4Fe-4S] proteins IspG and IspH in isoprenoid biosynthesis
… against Aquifex aeolicus IspH were discovered by compound library screening. The binding modes of both types of inhibitors have also been determined. The work reported here is of broad general interest, since it clarifies the nature of the reaction mechanisms of IspG and IspH catalyses, and opens …
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Genetic and Chemical Genetic Approaches to Shiga Toxin Inhibition
… relied on a high-throughput screen of a small compound library to identify potential inhibitors of Shiga toxin intracellular transport, as Shiga toxin is known to undergo a stepwise progression through host cells following endocytosis. This screen identified three compounds with distinct …
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Assays for lycosyltransferases
… assay (LDA) was optimised and validated for compound library screening. Additionally, the applicability of the LDA was investigated with three other GTs: bovine β1,4-galactosyltransferase, TcdB from Clostridium difficile and NGT from Actinobacillus <br/>pleuropneumoniae. The validated LDA was …
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Phosphoglycerate kinase 1 as a therapeutic target in motor neuron disease
… the most promising PGK1 activators from a compound library. These lead compounds were then screened in a C9orf72 knockdown zebrafish model of MND. This work highlighted the importance of using a disease model for screening, as adding extra PGK1 to cells with adequate levels shows little …
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Design and Synthesis of Inhibitors of Mycobacterium tuberculosis Menaquinone D (Mtb MenD) as Potential Therapeutics for Tuberculosis (Tb)
… N-oxide preparation enabled the assembly of a compound library, to address potential issues of solubility, hydrogen bonding interactions in the allosteric site, and cross-membrane transport. Collaborative work across the multidisciplinary team is on-going, in order to establish a complete …
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Expression, Purification and Molecular Characterisation of Sideroflexin Proteins
… Based on the principle that interactions with compounds increase the stability of proteins, a compound library was screened in thermostability assays. The results show that human sideroflexin 5 binds zinc ions, which was confirmed subsequently by native mass spectrometry and elemental mass …
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Development and Characterization of a Novel Protein Stability Probe
… was piloted by screening a kinase inhibitor library to identify known and novel kinases that regulate MYC stability. The Venus probe was also validated with another short half-life protein, MCL-1. This validated stability probe was expanded to a cell system that models MYC-driven human breast …
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Synthesis of Novel Sulfonamide-Based Calpain Inhibitors and Their Potential as Anti-Tumor Agents
… X-ray crystal structure of the µ-calpain, NCI compound library was screened by virtual screening method and diazosulfonamide <strong>1 </strong>(<em>K</em>i = 1.0 ± 0.02 µM) was identified as a new nonpeptide competitive inhibitor of µ-calpain. Analogues of <strong>1 </strong>were synthesized …
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