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 209 for “"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
… 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 repressors, …
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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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Roles of Cytoplasmic Deacetylase Hdac6 in Oncogenic Tumorigenesis
… to transcriptional 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 …
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Clinical Pharmacology of MS-275, A Histone Deacetylase Inhibitor
… 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 non-compartmental …
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Involvement of Histone Deacetylase 4 (HDAC4) in Osteoclast Function
… 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 culture and in vivo mouse model systems indicated that HDAC7 and 9 are negative regulators of …
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The Nucleosome Remodelling & Deacetylase complex: Genome folding & transcriptional regulation
… gene expression. The Nucleosome Remodeling and Deacetylase (NuRD) complex is one of four major ATP-dependent chromatin remodeling complexes and has been shown to be crucial for early embryonic development, to maintain transcriptional heterogeneity and to modulate the physical dynamics of …
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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
… 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 deacetylation – are tightly regulated to coordinate the …
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The Role of Histone Deacetylase 6 Inhibition on Systemic Lupus Erythematosus
… 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 central …
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Postnatal Role for Histone Deacetylase 1 and 2 in Behavioral and Neuronal Homeostasis
… 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 acetylation and deacetylation in regulating the …
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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
… 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 of a …
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A new mass spectrometric assay of N8-acetylspermidine deacetylase and partial purification of the enzyme
… for the target N<sup>8</sup>-acetylspermidine deacetylase, a not-well-studied but essential enzyme in the polyamine interconversion and reutilization pathway.</p><p>The enzyme assay, based on mass spectrometric detection of a specific reaction product following sample introduction by flow …
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Targeting histone deacetylase (HDACs) enzymes with novel bisnaphthalimidopropyl derivatives (BNIPs) as alternative breast cancer therapies.
… 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 expression …
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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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