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 6 of 6 for “"Bromodomain inhibitor"”.
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Mechanistic and Therapeutic Insights for Epigenetic Regulation in Cancer Development
… with increased levels of chromatin regulator/BET bromodomain protein BRD4, and paradoxically, sensitivity and resistance to BET bromodomain inhibition with small molecule inhibitor JQ1. Indeed, genetic and pharmacological inhibition of BRD4 profoundly suppresses both growth and tumorigenesis of …
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Development and investigation of novel chemoselective processes in Pd and Cu catalysis
… of a range of diverse substrates and a BET bromodomain inhibitor. Chapter two will describe an investigation into the source of rate independent chemoselectivity in the CuAAC reaction. Chemoselectivity in the CuAAC reaction has chiefly been demonstrated through the use of either activated or …
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Role of epigenetics in hematopoietic stem cell development
… C646 (histone acetyltransferase, or HAT, inhibitor) and OICR9249 (WDR5 inhibitor), and the two eraser molecules, Ex-527 (Sirt1 inhibitor) and JIB-04 (bromodomain inhibitor), showed varying degrees of increasing HSC formation. Of these molecules, C646 created the most significant increase …
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Targeting Myc-driven tumours - BETing on ATR
… a novel and orally bio-available BET bromodomain inhibitor (BETi) RVX2135. We also identified BET bromodomain proteins as a valuable therapeutic target against MYC driven tumours in vitro and in vivo. Gene expression profiling to identify these transcriptional changes enabled us to …
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Predictive Modelling of the Primary and Secondary Pharmacology of Compounds in Drug Discovery
… models, on the same bioactivity dataset for the bromodomain-containing proteins. Furthermore, we established the applicability domain of the model by employing conformal prediction, which was further used to aid the selection of compounds for prospective experimental testing in bromodomain …
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Investigation of novel therapeutic strategies in B cell and antibody mediated disease
… study investigating the potential efficacy of bromodomain inhibitors in reducing antibody-mediated immune cell activation. Immune complexed antigen can activate mononuclear phagocytes (MNP), comprising macrophages and dendritic cells (DCs), via ligation of Fc gamma receptors (FcγR), that bind …