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histone acetylation

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https://www.readbyqxmd.com/read/28213432/targeting-cancer-cells-with-bet-bromodomain-inhibitors
#1
Yali Xu, Christopher R Vakoc
Cancer cells are often hypersensitive to the targeting of transcriptional regulators, which may reflect the deregulated gene expression programs that underlie malignant transformation. One of the most prominent transcriptional vulnerabilities in human cancer to emerge in recent years is the bromodomain and extraterminal (BET) family of proteins, which are coactivators that link acetylated transcription factors and histones to the activation of RNA polymerase II. Despite unclear mechanisms underlying the gene specificity of BET protein function, small molecules targeting these regulators preferentially suppress the transcription of cancer-promoting genes...
February 17, 2017: Cold Spring Harbor Perspectives in Medicine
https://www.readbyqxmd.com/read/28213282/design-synthesis-and-biological-evaluation-of-thienopyrimidine-hydroxamic-acid-based-derivatives-as-structurally-novel-histone-deacetylase-hdac-inhibitors
#2
Jiang Wang, Mingbo Su, Tingting Li, Anhui Gao, Wei Yang, Li Sheng, Yi Zang, Jia Li, Hong Liu
New thienopyrimidine hydroxamic acid derivatives as HDACs inhibitors were designed, synthesized and evaluated. All compounds were evaluated for their ability to inhibit recombinant human HDAC1, HDAC3, and HDAC6 isoforms and in vitro anti-proliferative activity on tumor cell lines RMPI 8226 and HCT 116. Most of these compounds displayed good to excellent inhibitory activities against HDACs. The IC50 values of compound 9m against HDAC1, HDAC3, and HDAC6 was 29.81 ± 0.52 nM, 24.71 ± 1.16 nM, and 21.29 ± 0...
January 23, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28212902/intrauterine-valproate-exposure-is-associated-with-alterations-in-hippocampal-cell-numbers-and-folate-metabolism-in-a-rat-model-of-valproate-teratogenicity
#3
Alexander Semmler, Christian Frisch, Christiane Bleul, Desiree Smith, Laurent Bigler, Jean-Christophe Prost, Henk Blom, Michael Linnebank
PURPOSE: Valproate is one of the most commonly used anticonvulsive drugs. Despite its significant benefits, the teratogenicity of valproate is a relevant problem in the treatment of women of childbearing age. In addition to major congenital malformations, such as neural tube defects, reduced intelligence and attention after intrauterine valproate exposure are reported. Until now the mechanisms of teratogenicity of VPA are poorly understood and concepts how to reduce valproate teratogenicity are lacking...
January 27, 2017: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/28212191/endothelial-cell-metabolism-an-update-anno-2017
#4
Laure-Anne Teuwen, Nihed Draoui, Charlotte Dubois, Peter Carmeliet
PURPOSE OF REVIEW: Endothelial cell metabolism has recently emerged as an important coregulator of angiogenesis and is therefore a promising new target in various angiogenesis-associated illnesses, like cancer. In this review, we discuss recent insights in endothelial cell metabolism in both physiological and pathological conditions and discuss possible translational implications. RECENT FINDINGS: Two metabolic pathways that determine the performance of endothelial cells are glycolysis and fatty acid oxidation (FAO)...
February 15, 2017: Current Opinion in Hematology
https://www.readbyqxmd.com/read/28205129/remifentanil-postconditioning-ameliorates-histone-h3-acetylation-modification-in-h9c2-cardiomyoblasts-after-hypoxia-reoxygenation-via-attenuating-endoplasmic-reticulum-stress
#5
Manli Chen, Qin Liu, Lijian Chen, Lei Zhang, Erwei Gu
Remifentanil postconditioning (RPC) elicits cardioprotection against ischemia/reperfusion injury (IRI) by attenuating apoptosis associated with endoplasmic reticulum stress (ERS). Histone H3, acetylation modifications of histone H3, and histone deacetylases (HDAC) also have key roles in the mediation of the survival and apoptosis of cardiomyocytes. In this study, an in vitro IRI model was established with H9c2 cardiomyoblasts to investigate the role of histone H3 acetylation and HDAC3 in RPC-induced attenuation of ERS-associated apoptosis...
February 16, 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28202522/histone-acetyltransferase-activity-of-mof-is-required-for-mll-af9-leukemogenesis
#6
Daria G Valerio, Haiming Xu, Chun-Wei Chen, Takayuki Hoshii, Meghan E Eisold, Christopher Delaney, Monica Cusan, Aniruddha J Deshpande, Chun-Hao Huang, Amaia Lujambio, Y George G Zheng, Johannes Zuber, Tej K Pandita, Scott W Lowe, Scott A Armstrong
Chromatin-based mechanisms offer therapeutic targets in acute myeloid leukemia (AML) that are of great current interest. In this study, we conducted an RNAi-based screen to identify druggable chromatin regulator-based targets in leukemias marked by oncogenic rearrangements of the MLL gene. In this manner, we discovered the H4K16 histone acetyltransferase (HAT) MOF to be a potent suppressor of leukemia cell growth. Conditional deletion of Mof in a mouse model of MLL-AF9-driven leukemogenesis reduced tumor burden and prolonged host survival...
February 15, 2017: Cancer Research
https://www.readbyqxmd.com/read/28195723/drug-discovery-targeting-bromodomain-containing-protein-4-brd4
#7
Zhiqing Liu, Pingyuan Wang, Haiying Chen, Eric A Wold, Bing Tian, Allan R Brasier, Jia Zhou
BRD4, the most extensively studied member of BET family, is an epigenetic regulator that localizes to DNA via binding acetylated histones and controls the expression of therapeutically important gene regulatory networks through recruiting transcription factors to form mediator complexes, phosphorylating RNA polymerase II and by its intrinsic histone acetyltransferase activity. Disrupting the protein-protein interactions between BRD4 and acetyl-lysine has been shown to effectively block cell proliferation in cancer, cytokine production in acute inflammation, etc...
February 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28195362/low-intensity-ultrasound-enhances-histone-acetylation-and-inhibition-of-interleukin-6-messenger-rna-expression-by-the-histone-deacetylase-inhibitor-sodium-butyrate-in-fibroblasts
#8
Noriaki Maeshige, Yuka Koga, Masayuki Tanaka, Michiko Aoyama-Ishikawa, Makoto Miyoshi, Makoto Usami, Hidemi Fujino
OBJECTIVES: Sodium butyrate, an inhibitor of histone deacetylase, has several therapeutic actions, including anti-inflammation. These actions depend on the concentration of sodium butyrate. In addition, lower concentrations have shown no effect on inflammation. Sonoporation by ultrasound can modify the permeability of the cell plasma membrane. Thus, the effects of sodium butyrate may be enhanced by the ultrasonic acoustics. Therefore, the facilitative effects of low-intensity ultrasound on histone acetylation and interleukin 6 (IL-6) regulation by sodium butyrate were investigated in this study...
February 3, 2017: Journal of Ultrasound in Medicine: Official Journal of the American Institute of Ultrasound in Medicine
https://www.readbyqxmd.com/read/28194469/phenylephrine-induced-cardiac-hypertrophy-is-attenuated-by-a-histone-acetylase-inhibitor-anacardic-acid-in-mice
#9
Chang Peng, Xiaomei Luo, Shuo Li, Huichao Sun
Cardiac hypertrophy is a complex process involving highly coordinated but tight regulation of multiple elements, such as in epigenetics, which make an important contribution to myocardium remodeling and cardiac hypertrophy. Epigenetic regulations, particularly histone acetylation, have been implicated in cardiac hypertrophy, however, the exact mechanism is still largely unknown. In the present study, we explored the potential attenuating effects of Chinese herbal extract anacardic acid on phenylephrine-induced cardiac hypertrophy and the underlying mechanism...
February 14, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28192414/selective-in-vivo-metabolic-cell-labeling-mediated-cancer-targeting
#10
Hua Wang, Ruibo Wang, Kaimin Cai, Hua He, Yang Liu, Jonathan Yen, Zhiyu Wang, Ming Xu, Yiwen Sun, Xin Zhou, Qian Yin, Li Tang, Iwona T Dobrucki, Lawrence W Dobrucki, Eric J Chaney, Stephen A Boppart, Timothy M Fan, Stéphane Lezmi, Xuesi Chen, Lichen Yin, Jianjun Cheng
Distinguishing cancer cells from normal cells through surface receptors is vital for cancer diagnosis and targeted therapy. Metabolic glycoengineering of unnatural sugars provides a powerful tool to manually introduce chemical receptors onto the cell surface; however, cancer-selective labeling still remains a great challenge. Herein we report the design of sugars that can selectively label cancer cells both in vitro and in vivo. Specifically, we inhibit the cell-labeling activity of tetraacetyl-N-azidoacetylmannosamine (Ac4ManAz) by converting its anomeric acetyl group to a caged ether bond that can be selectively cleaved by cancer-overexpressed enzymes and thus enables the overexpression of azido groups on the surface of cancer cells...
February 13, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/28191871/distinct-modes-of-smad2-chromatin-binding-and-remodeling-shape-the-transcriptional-response-to-nodal-activin-signaling
#11
Davide M Coda, Tessa Gaarenstroom, Philip East, Harshil Patel, Daniel S J Miller, Anna Lobley, Nik Matthews, Aengus Stewart, Caroline S Hill
NODAL/Activin signaling orchestrates key processes during embryonic development via SMAD2. How SMAD2 activates programs of gene expression that are modulated over time however, is not known. Here we delineate the sequence of events that occur from SMAD2 binding to transcriptional activation, and the mechanisms underlying them. NODAL/Activin signaling induces dramatic chromatin landscape changes, and a dynamic transcriptional network regulated by SMAD2, acting via multiple mechanisms. Crucially we have discovered two modes of SMAD2 binding...
February 13, 2017: ELife
https://www.readbyqxmd.com/read/28188175/gcn5-determines-the-fate-of-drosophila-germline-stem-cells-through-degradation-of-cyclin-a
#12
Tianqi Liu, Qi Wang, Wenqing Li, Feiyu Mao, Shanshan Yue, Sun Liu, Xiaona Liu, Shan Xiao, Laixin Xia
The fluctuating CDK-CYCLIN complex plays a general role in cell-cycle control. Many types of stem cells use unique features of the cell cycle to facilitate asymmetric division. However, the manner in which these features are established remains poorly understood. The cell cycle of Drosophila female germline stem cells (GSCs) is characterized by short G1 and very long G2 phases, making it an excellent model for the study of cell cycle control in stem cell fate determination. Using a Drosophila female GSCs model, we found Gcn5, the first discovered histone acetyltransferase, to maintain germline stem cells in Drosophila ovaries...
February 10, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28187447/egr-1-and-rna-pol-ii-facilitate-glioma-cell-gdnf-transcription-induced-by-histone-hyperacetylation-in-promoter-ii
#13
Bao-Le Zhang, Ting-Wen Guo, Le-Le Gao, Guang-Quan Ji, Xiao-He Gu, Yu-Qi Shao, Rui-Qin Yao, Dian-Shuai Gao
The specific mechanisms for epigenetic regulation of gene transcription remain to be elucidated. We previously demonstrated that hyperacetylation of histone H3K9 in promoter II of glioma cells promotes high transcription of the glial cell line-derived neurotrophic factor (GDNF) gene. This hyperacetylation significantly enhanced Egr-1 binding and increased the recruitment of RNA polymerase II (RNA POL II) to that region (P < 0.05). Egr-1 expression was abnormally increased in C6 glioma cells. Further overexpression of Egr-1 significantly increased Egr-1 binding to GDNF promoter II, while increasing RNA POL II recruitment, thus increasing GDNF transcription (P < 0...
February 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28185898/sirt2-inhibition-modulate-glutamate-and-serotonin-systems-in-the-prefrontal-cortex-and-induces-antidepressant-like-action
#14
Mercedes Erburu, Irene Muñoz-Cobo, Teresa Díaz-Perdigon, Paolo Mellini, Takayoshi Suzuki, Elena Puerta, Rosa M Tordera
Growing evidence suggests that changes in histone acetylation in specific sites of the chromatin modulate neuronal plasticity and contribute to antidepressant-like action. Sirtuin 2 (SIRT2) is a class III NAD(+)-dependent histone deacetylase involved in transcriptional repression of genes regulating synaptic plasticity. Importantly, a key role for the glutamate system in prefrontal cortex (PFC) synaptic plasticity changes induced by antidepressants has been suggested. Here, we asked whether SIRT2 could be a pharmacological target for depression therapy...
February 6, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28185826/chaetocin-a-histone-methyltransferase-inhibitor-impairs-proliferation-arrests-cell-cycle-and-induces-nucleolar-disassembly-in-trypanosoma-cruzi
#15
Aline Araujo Zuma, Jean de Oliveira Santos, Isabela Mendes, Wanderley de Souza, Carlos Renato Machado, E Maria Cristina M Motta
The Trypanosomatidae family includes pathogenic species of medical and veterinary interest. Chagas disease is endemic in Latin America, and about 8 million people are infected worldwide. There is a need for more effective drugs for the acute, undetermined and chronic phases of the disease that, in addition, do not cause side effects, stimulating the search for identification of new drug targets, as well as new chemotherapeutic targets. Trypanosomatids contain characteristic structures, such as the nucleus that undergoes a closed mitosis without chromosome formation and variations of chromatin packing in the different protozoa developmental stages...
February 6, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28182198/a-time-series-analysis-of-altered-histone-h3-acetylation-and-gene-expression-during-the-course-of-mmaiii-induced-malignant-transformation-of-urinary-bladder-cells
#16
Jinqiu Zhu, Jie Wang, Xushen Chen, Maria Tsompana, Daniel Gaile, Michael Buck, Xuefeng Ren
No abstract text is available yet for this article.
February 9, 2017: Carcinogenesis
https://www.readbyqxmd.com/read/28180300/epigenetic-changes-in-histone-acetylation-underpin-resistance-to-the-topoisomerase-i-inhibitor-irinotecan
#17
Cornelia Meisenberg, Mohamed E Ashour, Lamia El-Shafie, Chunyan Liao, Adam Hodgson, Alice Pilborough, Syed A Khurram, Jessica A Downs, Simon E Ward, Sherif F El-Khamisy
No abstract text is available yet for this article.
February 17, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28179408/time-resolved-global-and-chromatin-proteomics-during-herpes-simplex-virus-hsv-1-infection
#18
Katarzyna Kulej, Daphne C Avgousti, Simone Sidoli, Christin Herrmann, Ashley N Della Fera, Eui Tae Kim, Benjamin A Garcia, Matthew D Weitzman
Herpes simplex virus (HSV-1) lytic infection results in global changes to the host cell proteome and the proteins associated with host chromatin. We present a system level characterization of proteome dynamics during infection by performing a multi-dimensional analysis during HSV-1 lytic infection of human foreskin fibroblast (HFF) cells. Our study includes identification and quantification of the host and viral proteomes, phosphoproteomes, chromatin bound proteomes and post-translational modifications (PTMs) on cellular histones during infection...
February 8, 2017: Molecular & Cellular Proteomics: MCP
https://www.readbyqxmd.com/read/28177898/maternal-dietary-zinc-supplementation-enhances-the-epigenetic-activated-antioxidant-ability-of-chick-embryos-from-maternal-normal-and-high-temperatures
#19
Yongwen Zhu, Xiudong Liao, Lin Lu, Wenxiang Li, Liyang Zhang, Cheng Ji, Xi Lin, Hsiao-Ching Liu, Jack Odle, Xugang Luo
The role of maternal dietary zinc supplementation in protecting the embryos from maternal hyperthermia-induced negative effects via epigenetic mechanisms was examined using an avian model (Gallus gallus). Broiler breeder hens were exposed to two maternal temperatures (21°C and 32°C) × three maternal dietary zinc treatments (zinc-unsupplemented control diet, the control diet + 110 mg zinc/kg inorganic or organic zinc) for 8 weeks. Maternal hyperthermia increased the embryonic mortality and induced oxidative damage evidenced by the elevated mRNA expressions of heat shock protein genes...
February 3, 2017: Oncotarget
https://www.readbyqxmd.com/read/28176832/epro-clearsee-a-simple-immunohistochemical-method-that-does-not-require-sectioning-of-plant-samples
#20
Kiyotaka Nagaki, Naoki Yamaji, Minoru Murata
Investigations into the epigenetic status of individual cells within tissues can produce both epigenetic data for different cell types and positional information of the cells. Thus, these investigations are important for understanding the intra- and inter-cellular control systems of developmental and environmental responses in plants. However, a simple method to detect epigenetic modifications of individual cells in plant tissues is not yet available because detection of the modifications requires immunohistochemistry using specific antibodies...
February 8, 2017: Scientific Reports
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