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 18 of 18 for “"HDAC inhibition"”.
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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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Dual mTOR/HDAC Inhibition: Preclinical Development of a Novel Breast Cancer Therapy
… despite effective upstream receptor inhibition. Activation of this pathway increases ribosome biogenesis and translation of oncogenic mRNAs, which are controlled by intracellular histone deacetylase (HDAC) activity as well. In fact, HDAC inhibitors that have been implemented into …
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Delineating mechanisms which underlie differential cell fates induced by p53 activation and HDAC inhibition in colorectal cancer
… demonstrated that combination of direct (MDM2 inhibition) or indirect (DNA-damaging chemotherapy) p53 activation with inhibitors of nuclear Class-I Histone deacetylases (HDACi) is effective in enhancing p53- dependent apoptotic cell death in multiple models of CRC. Interestingly, despite a …
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HDAC inhibition results in suppression of FOXM1 and genes associated with poor prognosis prostate cancer through p53 dependent and independent mechanisms
… also known to be suppressed by p53. <br/><br/>HDACi are an emerging class of epigenetic modifying anti-cancer agents that we hypothesise will enhance p53 mediated cell death, whilst also altering patterns of gene expression to target p53-dependent and independent vulnerabilities in PCa. Using …
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Modulation of Histone Deacetylases Attenuates the Pathogenesis of Alzheimer's disease
… (HAT) und Histon-Deacetylasen (HDAC) reguliert. Diese Arbeit zeigt, dass eine Erhöhung der Histonacetylierung durch HDAC-Inhibition die Kognition im AD-Mausmodell verbessert. Dies beinhaltet insb! esondere die erhöhte Expression der Gene, die bei der Gedächtnisbildung von …
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Quantitative approaches to probe the acetylproteome
… Furthermore, we demonstrated that short-term HDAC inhibition alters phosphotyrosine-signaling networks. To better understand this behavior, a suite of biochemical and computational methods were developed. Bromodomains were engineered to explore binding preferences using degenerate peptide …
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Valproic Acid Disrupts Hematopoiesis in Xenopus Laevis Through the Inhibition of Histone Deacetylase 3.
Histone deacetylases (HDACs) are important regulators of developmental processes and cellular functions. However, their role in hematopoiesis has not been determined, and in Xenopus laevis, a specific function for HDACs has yet to be identified. In the present work, we employed the class I …
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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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The development and validation of a novel patient-derived 3D meningioma cell culture model
… tyrosine kinase (MERTK) and histone deacetylase (HDAC) inhibition, which in addition to having a synergistic inhibitory effect on spheroid viability, also decreased spheroid proliferation, expression of EMT-associated proteins and spheroid invasion capacity. Hence, I propose this meningioma …
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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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The Role of Histone Deacetylases in Cytokine Regulation in Human Gestational Tissues
… little is known about histone deacetylases (HDACs) in the placenta and membranes. The overall aim of this research was to investigate the role of histone deacetylases in cytokine regulation in human gestational tissues. HDAC expression was characterised in term placental, amnion and …
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Characterization of a Novel NPC1I1061T Knock-in Mouse Model of Niemann-Pick Type C1 Disease
… mutation. Histone deacetylase (HDAC) inhibitors have also been shown to augment NPC1<super>I1061T</super> protein and cholesterol egress from the lysosome, possibly via an increase in HSP90 expression. Together, these findings raise the possibility that small molecule-based …
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Insights into the molecular mechanisms of function and regulation of histone crotonylation
… processes – the class I histone deacetylases (HDACs). I further characterise how its genome-wide localisation pattern is influenced by HDAC inhibition and compare it to acetylation. Pivotal for our understanding of histone crotonylation is the identification of 'reader' molecules, which are …
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Novel bisnaphthalimidopropyl polyamine derivatives: their mode of action in a breast cancer cell system.
… Interestingly, BNIPDaCHM was identified, using HDAC assay kits, as a potent and selective SIRT2 enzyme inhibitor, thus, identifying, a novel structural backbone for the selective inhibition of HDAC enzymes.
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Targeting histone deacetylase (HDACs) enzymes with novel bisnaphthalimidopropyl derivatives (BNIPs) as alternative breast cancer therapies.
… Moreover, BNIPs inhibited histone deacetylases (HDAC) activity after 24 hours treatment in MDA-MB-231 and SKBR-3 cells and BNIPDaCHM was identified as a potential SIRT2 inhibitor, in SKBR-3 cells. According to Proteome Profiler Arrays, BNIPDaCHM and BNIPPiEth altered the expression of cell …
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Integration of class 1 HDAC inhibitors into current treatments for prostate cancer
… regulators, including histone deacetylases (HDAC), are commonly mutated and highly expressed in cancer, representing attractive clinical targets. Although five HDAC inhibitors (HDACi) have been FDA approved for myelodysplastic syndromes, evaluation of pan-HDACi in CaP clinical trials as …
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Targeting Histone Deacetylases (Hdac) For The Treatment of Soft Tissue Sarcoma
<p><strong>Targeting Histone deacetylases (HDAC) for the </strong><strong>treatment of genetically complex soft tissue sarcoma</strong></p> <p>Histone deactylase inhibitors (HDACi) are a new class of anticancer therapeutics; however, little is known about HDACi or the individual contribution of …
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Defining the potential of HDAC5 and HDAC9 as therapeutic targets for Parkinson’s disease
… the development of new therapies. The targeted inhibition of histone deacetylases (HDACs), enzymes which regulate histone acetylation, have shown some promise in this regard. For example, pan-HDAC inhibition by pharmacological compounds in PD models have been reported to provide some …