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 44 for “"HDAC INHIBITORS"”.
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Integration of class 1 HDAC inhibitors into current treatments for prostate cancer
… prostate cancer (CRPC). Androgen signalling inhibitors (ASI), including Enzalutamide (ENZ) and Abiraterone (ABI), are effective treatments for metastatic CRPC however, resistance develops within 24-months of initial exposure in the majority of patients. <br/><br/>Epigenetic silencing of …
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Development Of Elisa-Based Hdac Activity Assay For Identification Of Isoform Selective Hdac Inhibitors
… drugs that inhibit histone deacetylase (HDAC) proteins. HDACs are histone modifying enzymes that regulate transcription of genes. Aberrant recruitment of HDACs to the transcription factors leads to tumor onset and growth. Because of their potential anti-cancer therapeutic interest, …
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The structural requirements of histone deacetylase (hdac) inhibitors: suberoylanilide hydroxamic acid (saha) analogues modified at c3, c6, and c7 positions enhance selectivity
<p>Histone deacetylase (HDAC) proteins are targets for drug design towards the treatment of cancers since overexpression of HDAC is linked to cancer. Several HDAC inhibitors, including the FDA approved drug suberoylanilide hydroxamic acid (SAHA, Vorinostat), have cleared clinical trials and emerged …
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Development of chemical inducers of dimerization for screening competitive histone deactelyase inhibitors
<p>Histone Deacetylase (HDAC) proteins are transcriptional regulators that affect histone proteins, which are involved in packaging of DNA into chromosomes. HDACs have been linked to the proliferation of cancer through their role in transcriptional regulation. Due to these findings, HDAC inhibitors …
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Identification of substrate-selective histone deacetylases and their inhibitors that mediate HER2 transcript stability
… include the utilization of histone deacetylase (HDAC) inhibitors. It has been observed that HDAC inhibitors can induce the rapid decay of oncogenic transcripts such as the HER2 mRNA, though the mechanism underlying this process remains undefined. Earlier observations in our lab led to speculation …
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Investigation of the Role of Histone Acetylation in Hippocampus-Dependent Memory Formation
… pharmacologically blocking histone deacetylases (HDAC) enhances long-term memory formation. Memory enhancement by HDAC inhibitors requires the interaction between the transcription factor CREB and CBP, suggesting that these two processes converge at functionally relevant target genes. As reviewed …
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Evaluation of inhibitors of histone deacetylases as potential neurotrophic agents
<p>The inhibitors of histone deacetylases (HDACs) have shown promising neuroprotective and neuroactive properties. A set of pan- and isoform-specific HDAC inhibitors were evaluated for neurotrophic activity on Neuroscreen-1 (NS-1) cells, a subclone of PC-12 (rat pheochromocytoma) cells. </p> <p>The …
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The role of c-FLIP in regulating resistance to ionizing radiation
… to radiotherapy. <br/><br/> Clinically approved HDAC inhibitors were used to down regulate FLIP protein levels, and the effect on IR-induced cell death was assessed. The results presented in this study reveal that F1DAC inhibitors sensitize non-small cell lung carcinoma (NSCLC) cell lines to IR. …
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Can changes in SR protein acetylation affect alternative splicing?
… cell line was increased by histone deacetylase (HDAC) inhibition, using the HDAC inhibitors MS-275 and SAHA. RNA from treated cells was isolated for use with RT-PCR arrays developed by Peter Stoilov. Western blotting was used to determine efficacy of HDAC inhibitors on total cellular acetylation. …
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Function and Regulation of Phosphatidylinositol 3,4,5-Triphosphate-Dependent Rac Exchanger 1 (P-Rex1) in Cancer
… prostate cancer cells. Histone deacetylase (HDAC) inhibitors or silence of endogenous HDAC1 and HDAC2 markedly elevated P-Rex1 transcription in non-metastatic prostate cancer cells, whereas overexpression of recombinant HDAC1 in metastatic prostate cancer cells suppressed P-Rex1 expression. …
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Dual mTOR/HDAC Inhibition: Preclinical Development of a Novel Breast Cancer Therapy
… controlled by intracellular histone deacetylase (HDAC) activity as well. In fact, HDAC inhibitors that have been implemented into clinical practice are capable of overcoming resistance to HER2 and ER targeted therapeutics, in part by inducing the degradation of oncogenic transcripts. Given this …
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Roles of Cytoplasmic Deacetylase Hdac6 in Oncogenic Tumorigenesis
… repression. Moreover, histone deacetylase inhibitors induce growth arrest, differentiation and apoptosis of cancer cells and therefore appear to be promising anti-tumor agents. While transcriptional deregulation is thought to be the main mechanism underlying their therapeutic effects, the …
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EBV-Associated Gastric Cancer: From Initial Infection to Unique Therapeutic Approaches
… reactivation potential to histone deacetylase (HDAC) inhibitors and generated preclinical data supporting the use of HDAC inhibitors and the anti-viral ganciclovir for treatment of EBV+ epithelial tumors. Lastly, I have identified modulators of the response to a PI3Ka inhibitor in PIK3CA mutant …
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A mechanistic assessment of novel anticancer drugs targeting the metastatic cascade and tumour vascularisation.
… were shown to combine histone deacetylase (HDAC) inhibition with synergistic effects of the 4,5-diarylimidazole residue. Some of the derivatives proved a greater cytotoxicity against a panel of resistant cell lines and a higher specificity for cancer over non-malignant cells then the …
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Investigating the pathogenesis and therapy of Friedreich Ataxia
… compounds and class III histone deacetylase (HDAC) inhibitors. Although DNA demethylating agents showed increased FXN expression, no correlation between the level of DNA methylation and FXN expression was identified. Nevertheless, the use of GAA interacting compounds, particularly DB221, and …
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Isoform-Selective HDAC Inhibition for the Treatment of Lupus Nephritis
… to contribute to disease. Histone deacetylases (HDACs) are a class of enzymes that hydrolyze the lysine bound acetyl group in both histone and non-histone proteins thereby altering protein structure and function. While the use of pan-HDAC inhibitors has proven to be effective for the treatment of …
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Impaired Control of Chronic Herpesvirus Infection in Tissue Resident Macrophages During Coinfection with Intestinal Parasite and Other Cell-intrinsic Herpesvirus Interactions
… can be caused by a variety of signals, such as HDAC inhibitors. While some of these signals are known, it is still unclear whether there are cell-specific reactivation mechanisms, and if so, which signals cause them. Further, human gammaherpesviruses are endemic in areas that also have a high …
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Leveraging Single Cell Technologies For The Characterization and Treatment of Refractory Pancreatic Cancer
… of epigenetically-modifying therapeutic agents (HDAC inhibitors). I describe a novel HDACi resistance mechanism of AP1 activation, which can be intercepted by using an AP1 inhibitor in combination with an HDAC inhibitor to achieve tumor cell death. Finally, in an effort to explore and …
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Microbiota regulate short chain fatty acids and influence histone acylations in intestinal epithelial cells.
… I identified that class I histone deacetylases (HDACs) are efficient histone decrotonylases. I have achieved this through a combination of biological analysis of the effects of treatment with HDAC inhibitors and in vitro analysis of purified proteins, which enabled determination of kinetic …
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Uncovering The Zeb1 Interactome to Identify Novel Regulators of Metastatic Non-Small Cell Lung Cancer
… amongst ZEB1 and the histone deacetylase (HDAC)-containing nucleosome and deacetylase remodeling complex (NuRD). Through treatment with class I HDAC inhibitors Trichostatin A, we identified that ZEB1 homodimerizes and determine that acetylation at lysine residue 811 regulates this …
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