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 162 for “"Histone Deacetylase"”.
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Discovery of Isozyme Selective Histone Deacetylase Inhibitors.
Discovery of Isozyme Selective Histone Deacetylase Inhibitors.
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EFFECTS OF HISTONE DEACETYLASE INHIBITORS ON ENERGY METABOLISM
… involving enzymes, such as members of the histone deacetylase (HDAC) family, in particular those belonging to class I and class II, which modulate post-translational modifications on target proteins. The current knowledge on HDACs is that they function in general as transcriptional …
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Histone Deacetylase 1: Mutagenesis And Small Molecule Studies
<p>Histone deacetylase 1 (HDAC1) has been linked to cell growth and cell cycle regulation, which makes it a widely recognized target for anticancer drugs. The 14 Å channel of Class 1 HDAC isotypes has long being hypothesized to be the exit cavity for acetate following deacetylation. The amino acids …
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Clinical Pharmacology of MS-275, A Histone Deacetylase Inhibitor
… and plasma protein binding of MS-275, a novel histone deacetylase inhibitor, in patients with solid tumors and lymphomas. A validated LC/MS assay was developed to quantitate MS-275 in plasma, human liver microsomes and urine. The pharmacokinetic (PK) evaluation was done using a …
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Involvement of Histone Deacetylase 4 (HDAC4) in Osteoclast Function
… develop effective therapies for bone disorders. Histone deacetylation is one such potential mechanism. It has been reported that class IIa histone deacetylase (HDAC), which include HDAC4, 5, 7 and 9 are regulators of osteoclastogenesis. Evidence from our lab and other labs using in vitro cell …
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Regulation of neuronal genomic integrity through histone deacetylase cooperativity
… I characterize the functions of two lysine deacetylases, SIRT1 and HDAC1, in the neuronal response to DNA double strand breaks (DSBs). Both SIRT1 and HDAC1 were previously shown to promote neuronal survival in a mouse model of neurodegeneration in which the appearance of DSBs precedes other …
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Histone Deacetylase 7 and Transcriptional Regulatory Networks of the Vascular Endothelium
… either facilitate or inhibit gene transcription. Histone acetyltransferases (HATs) and histone deacetylases (HDACs) are two such classes of enzymes that regulate the epigenetic code. Their opposing actions – to activate transcription by histone acetylation and to inhibit transcription by …
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The Role of Histone Deacetylase 6 Inhibition on Systemic Lupus Erythematosus
… to replace or reduce the use of current ones. Histone deacetylase 6 (HDAC6) plays a variety of biologic functions in a number of important molecular pathways in diverse immune cells. Both innate and adaptive immune cells contribute to pathogenesis of lupus. Among those cells, B cells play a …
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Postnatal Role for Histone Deacetylase 1 and 2 in Behavioral and Neuronal Homeostasis
… without alterations in the DNA sequence. Histone acetyltransferases (HATs) and histone deacetylases (HDACs) can influence gene activity by inducing either an active or inactive chromatin state, respectively. Accumulating in vitro data has demonstrated a crucial function for histone …
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Oxidative Stress Based Strategies For Enhancing The Efficacy of Histone Deacetylase Inhibitors (Hdaci)
<p>Histone deacetylase inhibitors (HDACi) are anti-cancer drugs that primarily act upon acetylation of histones, however they also increase levels of intracellular reactive oxygen species (ROS). We hypothesized that agents that cause oxidative stress might enhance the efficacy of HDACi. To test …
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Structural Studies of Two Related Metallohydrolases: Human Histone Deacetylase 8 and Malarial Arginase
Metal-dependent histone deacetylases (HDACs) catalyze the deacetylation of lysine residues in histones and other proteins in eukaryotic cells. Isozyme HDAC8 is perhaps the archetypical member of the class I HDAC family and serves as a paradigm for studying structure-function relationships. We …
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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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CYCLIZATION-BASED SITE-SELECTIVE N-TERMINAL CYSTEINE CONJUGATION, PEPTIDE STAPLING AND HISTONE DEACETYLASE (HDAC) PROBING
… in monitoring the real-time activity of histone deacetylases (HDACs).
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STUDY ON HISTONE DEACETYLASE 3 AND ITS PHARMACOLOGICAL REGULATION IN THE PATHOPHYSIOLOGY OF ADIPOSE TISSUE
… both physiological and pathological conditions. Histone deacetylases (HDACs) are epigenome modifiers regulating adipocyte metabolism. Our previous studies with chemical inhibitors or genetic alterations of HDAC3 have shown metabolic rewiring of white adipocytes towards browning via the activation …
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Targeting histone deacetylase (HDACs) enzymes with novel bisnaphthalimidopropyl derivatives (BNIPs) as alternative breast cancer therapies.
… and SKBR-3 cells. 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 …
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Receptor-Mediated Hypertrophic Signaling Via Protein Kinase D and Histone Deacetylase 5 in Adult Myocytes
<p>Hemodynamic stress and neurohumoral signaling are common causes of cardiac hypertrophy. These extrinsic stress stimuli typically act on GPCR and induce a cascade of signal transduction to re-program terminally differentiated myocytes to grow in length or width. The compensatory hypertrophic …
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The Role of the Nucleosome Remodeling and Histone Deacetylase (NuRD) Complex in Fetal γ-Globin Expression
<p>An understanding of the human fetal to adult hemoglobin switch offers the potential to ameliorate β-type globin gene disorders such as sickle cell anemia and β-thalassemia through activation of the fetal γ-globin gene. Chromatin modifying complexes, including MBD2-NuRD and GATA-1/FOG-1/NuRD play …
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The synergistic interaction between CD20 monoclonal antibodies and Histone Deacetylase inhibitors in B cell Non Hodgkin’s Lymphoma
… patients with B cell Non Hodgkin’s<br/>lymphoma. Histone deacetylase inhibitors are a novel class of anti cancer<br/>agents targeting epigenetic regulation.<br/><br/>This thesis addresses the interaction between histone deacetylase inhibitors<br/>and anti-CD20 monoclonal antibodies, including …
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Epigenetics of Neurodegeneration: Quantification of Histone Deacetylase Isoforms and Post-translational Modifications of Histones in Alzheimer’s Disease
Histone post-translational modifications have been implicated in many biological functions and diseases and serve an important role in epigenetic regulation of gene expression. Aberrant modulations in histone post-translational have been suggested to occur in the brain as part of Alzheimer’s …
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Histone deacetylase inhibitors as novel neuroprotective agents in in vitro and in vivo models of Parkinson’s disease
Histone deacetylases (HDAC) shift the balance towards chromatin condensation and silence gene expression. Aberrant recruitment of HDACs to alter transcription suggests the use of HDAC inhibitors (HDAC-Is) as potential therapeutic candidates for neurodegenerative disorders such as Parkinson’s …
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