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https://www.readbyqxmd.com/read/29687888/epigenetics-of-aberrant-cardiac-wound-healing
#1
Adam Russell-Hallinan, Chris J Watson, John A Baugh
Remodeling of cardiac tissue architecture is essential for normal organ development and maintaining homeostasis after injury. Injurious insults to the heart, such as hypertension and myocardial infarction, promote cellular responses including stimulation of resident inflammatory cells, activation of endothelial cells and recruitment of immune cells, hypertrophy of cardiomyocytes, and activation of fibroblasts. The physiological goal of this coordinated cellular response is to repair damaged tissue while maintaining or restoring cardiac contractile function...
March 26, 2018: Comprehensive Physiology
https://www.readbyqxmd.com/read/29685973/epigenetic-drug-discovery-a-success-story-for-cofactor-interference
#2
REVIEW
A Ganesan
Within the past two decades, seven epigenetic drugs have received regulatory approval and numerous other candidates are currently in clinical trials. Among the epigenetic targets are the writer and eraser enzymes that are, respectively, responsible for the reversible introduction and removal of structural modifications in the nucleosome. This review discusses the progress achieved in the design and development of inhibitors against the key writer and eraser pairs: DNA methyltransferases and Tet demethylases; lysine/arginine methyltransferases and lysine demethylases; and histone acetyltransferases and histone deacetylases...
June 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29685972/desferrioxamine-biosynthesis-diverse-hydroxamate-assembly-by-substrate-tolerant-acyl-transferase-desc
#3
Jade L Ronan, Nadia Kadi, Stephen A McMahon, James H Naismith, Lona M Alkhalaf, Gregory L Challis
Hydroxamate groups play key roles in the biological function of diverse natural products. Important examples include trichostatin A, which inhibits histone deacetylases via coordination of the active site zinc(II) ion with a hydroxamate group, and the desferrioxamines, which use three hydroxamate groups to chelate ferric iron. Desferrioxamine biosynthesis in Streptomyces species involves the DesD-catalysed condensation of various N -acylated derivatives of N -hydroxycadaverine with two molecules of N -succinyl- N -hydroxycadaverine to form a range of linear and macrocyclic tris-hydroxamates...
June 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29685969/isoform-selective-hdac1-6-8-inhibitors-with-an-imidazo-ketopiperazine-cap-containing-stereochemical-diversity
#4
Bertrand Lecointre, Remy Narozny, Maria Teresa Borrello, Johanna Senger, Alokta Chakrabarti, Manfred Jung, Martin Marek, Christophe Romier, Jelena Melesina, Wolfgang Sippl, Laurent Bischoff, A Ganesan
A series of hydroxamic acids linked by different lengths to a chiral imidazo-ketopiperazine scaffold were synthesized. The compounds with linker lengths of 6 and 7 carbon atoms were the most potent in histone deacetylase (HDAC) inhibition, and were specific submicromolar inhibitors of the HDAC1, HDAC6 and HDAC8 isoforms. A docking model for the binding mode predicts binding of the hydroxamic acid to the active site zinc cation and additional interactions between the imidazo-ketopiperazine and the enzyme rim...
June 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29685963/new-chemical-tools-for-probing-activity-and-inhibition-of-the-nad-dependent-lysine-deacylase-sirtuin-2
#5
Sören Swyter, Matthias Schiedel, Daria Monaldi, Sándor Szunyogh, Attila Lehotzky, Tobias Rumpf, Judit Ovádi, Wolfgang Sippl, Manfred Jung
Sirtuins are NAD+ -dependent protein deacylases capable of cleaving off acetyl as well as other acyl groups from the ɛ-amino group of lysines in histones and other substrate proteins. They have been reported as promising drug targets, and thus modulators of their activity are needed as molecular tools to uncover their biological function and as potential therapeutics. Here, we present new assay formats that complement existing assays for sirtuin biochemistry and cellular target engagement. Firstly, we report the development of a homogeneous fluorescence-based activity assay using unlabelled acylated peptides...
June 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29683269/multiple-machine-learning-based-chemoinformatics-models-for-identification-of-histone-acetyl-transferase-inhibitors
#6
Shagun Krishna, Sushil Kumar, Deependra Kumar Singh, Amar Deep Lakra, Dibyendu Banerjee, Mohammad Imran Siddiqi
The histone acetyl transferase (HAT) are involved in acetylation of histones that lead to transcription activation in numerous gene regulatory mechanisms. There are very few GCN5 HAT inhibitors reported despite of their role in cancer progression. In this study, we have utilized in-silico virtual screening approaches based on various machine learning algorithm to identify potent inhibitors of GCN5 HAT from commercially available Maybridge library. We have generated predictive chemoinformatics models based on k-Nearest neighbour, naïve Bayesian, Random Forest and Support Vector Machine...
April 23, 2018: Molecular Informatics
https://www.readbyqxmd.com/read/29682593/histone-deacetylase-inhibitor-based-chromatin-precipitation-for-identification-of-targeted-genomic-loci
#7
Thomas W Hanigan, Jeanne M Danes, Taha Y Taha, Jonna Frasor, Pavel A Petukhov
Histone deacetylase (HDAC) catalyzes the removal of acetyl marks from histones, effectively regulating gene expression. Genome wide chromatin immunoprecipitation (ChIP) studies have shown HDACs are present on numerous active and repressed genes. However, HDAC inhibitors (HDACi) only regulate a small subset of this population in a cell type dependent fashion. To determine genomic locations directly targeted by HDACi, we developed a chromatin precipitation method using a photoreactive HDAC inhibitor probe (photomate)...
2018: Journal of Biological Methods
https://www.readbyqxmd.com/read/29680858/relationship-between-histone-deacetylase-3-hdac3-and-breast-cancer
#8
Zhuhong Cui, Mingjun Xie, Zhenru Wu, Yujun Shi
BACKGROUND The modification of histone acetylation and deacetylation is the most important mechanism of chromatin remodeling. These modifications are a subset of epigenetic alterations which affect tumorigenesis and progression through changes in gene expression and cell growth. Results of histone modification studies prompted us to explore the therapeutic and prognostic significance of histone deacetylase 3 (HDAC3) expression in patients with breast cancer. MATERIAL AND METHODS Immunohistochemical (IHC) staining was used to detect HDAC3 expression in a tissue microarray (TMA) that included 145 patients diagnosed with invasive ductal breast carcinoma...
April 22, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/29679803/development-of-the-plant-derived-peptide-lunasin-as-an-anticancer-agent
#9
REVIEW
Saleha B Vuyyuri, Chris Shidal, Keith R Davis
The health benefits of soy consumption have long been recognized. An important potential benefit is the linkage of soy consumption with reduced cancer risk. One emerging factor that may confer the anticancer effects of soy is the peptide lunasin. Lunasin has both chemopreventive and therapeutic activities against a variety of carcinogens and cancer types. A novel feature of lunasin is that it contains multiple functional domains that can modulate gene expression through effects on histone acetylation and integrin signaling...
April 18, 2018: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/29679567/hdac-mediated-deacetylation-of-klf5-associates-with-its-proteasomal-degradation
#10
Ran Tao, Baotong Zhang, Yixiang Li, Jamie L King, Ruoyu Tian, Siyuan Xia, Cara Rae Schiavon, Jin-Tang Dong
Krüppel-like factor 5 (KLF5) is a basic transcription factor that regulates diverse cellular processes during tumor development. Acetylation of KLF5 at lysine 369 (K369) reverses its function from promoting to suppressing cell proliferation and tumor growth. In this study, we examined the regulation of KLF5 by histone deacetylases in the prostate cancer cell line DU 145. While confirming the functions of HDAC1/2 in KLF5 deacetylation and the promotion of cell proliferation, we found that the knockdown of HDAC1/2 upregulated KLF5 protein but not KLF5 mRNA, and the increase in KLF5 protein level by silencing HDAC1/2 was at least in part due to decreased proteasomal degradation...
April 18, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29679095/implication-of-the-vrk1-chromatin-kinase-in-the-signaling-responses-to-dna-damage-a-therapeutic-target
#11
REVIEW
Ignacio Campillo-Marcos, Pedro A Lazo
DNA damage causes a local distortion of chromatin that triggers the sequential processes that participate in specific DNA repair mechanisms. This initiation of the repair response requires the involvement of a protein whose activity can be regulated by histones. Kinases are candidates to regulate and coordinate the connection between a locally altered chromatin and the response initiating signals that lead to identification of the type of lesion and the sequential steps required in specific DNA damage responses (DDR)...
April 20, 2018: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/29677652/cardiomyocytes-have-mosaic-patterns-of-protein-expression
#12
Tony Y Wang, Dongwong Lee, Karen Fox-Talbot, Dan E Arking, Aravinda Chakravarti, Marc K Halushka
Skeletal myocytes have well-established fast and slow twitch fibers with unique gene and protein specific expression patterns. By immunohistochemical staining, these show a mosaic pattern across myocytes. We hypothesized cardiac myocytes may behave similarly where some proteins are differentially expressed between mature cardiomyocytes. We utilized the tool HPASubC on over 52,000 cardiac images of the Human Protein Atlas to identify differential protein expression patterns by immunohistochemistry across the cardiomyocytes...
March 24, 2018: Cardiovascular Pathology: the Official Journal of the Society for Cardiovascular Pathology
https://www.readbyqxmd.com/read/29676649/asbestos-induces-epigenetic-repression-of-ras-association-domain-containing-protein-1-p16-kinase-4a-inhibitor-and-p14-alternative-reading-frame-in-normal-human-mesothelial-cells
#13
Sichuan Xi, Eden C Payabyab, David M Straughan, Emily S Reardon, Mary Zhang, Julie A Hong, R Taylor Ripley, Chuong D Hoang, David S Schrump
RATIONALE: Whereas asbestos burden has been linked to cytogenetic alterations in malignant pleural mesotheliomas, epigenetic aberrations induced by these fibers have not been fully delineated. OBJECTIVES: The objective of this study was to establish an in vitro model to characterize early epigenetic events potentially contributing to malignant pleural mesothelioma. METHODS: Normal human mesothelial cells (LP9 and LP3) were cultured with or without crocidolite asbestos fibers (1 or 2 μg/cm2 ) for up to 10 days...
April 2018: Annals of the American Thoracic Society
https://www.readbyqxmd.com/read/29676637/epigenomic-alterations-and-gene-expression-profiles-in-human-respiratory-epithelial-cells-mediated-by-hookah-and-cigarette-smoke
#14
Yin Xiong, Sichuan Xi, Jigui Shan, Elvin Hekimoglu, Shih-Hsin Hsiao, Mary Zhang, Julie A Hong, Chris Tao, Haobin Chen, R Taylor Ripley, Chuong D Hoang, David S Schrump
RATIONALE: The effects of hookah smoke on respiratory epithelia have not been well characterized. OBJECTIVES: To characterize and compare the effects of hookah tobacco smoke and conventional cigarette smoke on the epigenome and transcriptome of human respiratory epithelia. METHODS: Normal human small airway epithelial cells and cyclin-dependent kinase 4/human telomerase reverse transcriptase-immortalized human bronchial epithelial cells were cultured for 5 days in normal media in the presence or absence of water pipe condensates or cigarette smoke condensates under relevant exposure conditions...
April 2018: Annals of the American Thoracic Society
https://www.readbyqxmd.com/read/29676588/lysine-acetyltransferase-inhibitors-structure-activity-relationships-and-potential-therapeutic-implications
#15
Francesco Fiorentino, Antonello Mai, Dante Rotili
Lysine acetylation is a post-translational modification of both histone and nonhistone proteins that is catalyzed by lysine acetyltransferases and plays a key role in numerous biological contexts. The dysregulation of this enzyme activity is implicated in many human pathologies such as cancer, neurological and inflammatory disorders. Many lysine acetyltransferase inhibitors (KATi) have been developed so far, but there is still the need for new, more potent, metabolically stable and selective KATi as chemical tools for studying KAT biology and/or as potential therapeutic agents...
April 20, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29675728/histone-deacetylase-2-inhibitor-cay10683-alleviates-lipopolysaccharide-induced-neuroinflammation-through-attenuating-tlr4-nf-%C3%AE%C2%BAb-signaling-pathway
#16
Fang-Zhou Jiao, Yao Wang, Hai-Yue Zhang, Wen-Bin Zhang, Lu-Wen Wang, Zuo-Jiong Gong
Neuroinflammation involves in the progression of many central nervous system diseases. Several studies have shown that histone deacetylase (HDAC) inhibitors modulated inflammatory responses in lipopolysaccharide (LPS) stimulated microglia. While, the mechanism is still unclear. The aim of present study was to investigate the effect of HDAC2 inhibitor CAY10683 on inflammatory responses and TLR4/NF-κB signaling pathways in LPS activated BV2 microglial cells and LPS induced mice neuroinflammation. The effect of CAY10683 on cell viability of BV2 microglial cells was detected by CCK-8 assay...
April 19, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29675133/benefit-of-oleuropein-aglycone-for-alzheimer-s-disease-by-promoting-autophagy
#17
REVIEW
Joaquín G Cordero, Ramón García-Escudero, Jesús Avila, Ricardo Gargini, Vega García-Escudero
Alzheimer's disease is a proteinopathy characterized by accumulation of hyperphosphorylated Tau and β -amyloid. Autophagy is a physiological process by which aggregated proteins and damaged organelles are eliminated through lysosomal digestion. Autophagy deficiency has been demonstrated in Alzheimer's patients impairing effective elimination of aggregates and damaged mitochondria, leading to their accumulation, increasing their toxicity and oxidative stress. In the present study, we demonstrated by microarray analysis the downregulation of fundamental autophagy and mitophagy pathways in Alzheimer's patients...
2018: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/29674394/acetyl-coa-promotes-glioblastoma-cell-adhesion-and-migration-through-ca-2-nfat-signaling
#18
Joyce V Lee, Corbett T Berry, Karla Kim, Payel Sen, Taehyong Kim, Alessandro Carrer, Sophie Trefely, Steven Zhao, Sully Fernandez, Lauren E Barney, Alyssa D Schwartz, Shelly R Peyton, Nathaniel W Snyder, Shelley L Berger, Bruce D Freedman, Kathryn E Wellen
The metabolite acetyl-coenzyme A (acetyl-CoA) is the required acetyl donor for lysine acetylation and thereby links metabolism, signaling, and epigenetics. Nutrient availability alters acetyl-CoA levels in cancer cells, correlating with changes in global histone acetylation and gene expression. However, the specific molecular mechanisms through which acetyl-CoA production impacts gene expression and its functional roles in promoting malignant phenotypes are poorly understood. Here, using histone H3 Lys27 acetylation (H3K27ac) ChIP-seq (chromatin immunoprecipitation [ChIP] coupled with next-generation sequencing) with normalization to an exogenous reference genome (ChIP-Rx), we found that changes in acetyl-CoA abundance trigger site-specific regulation of H3K27ac, correlating with gene expression as opposed to uniformly modulating this mark at all genes...
April 19, 2018: Genes & Development
https://www.readbyqxmd.com/read/29672823/developmental-disorders-with-intellectual-disability-driven-by-chromatin-dysregulation-clinical-overlaps-and-molecular-mechanisms
#19
REVIEW
L Larizza, P Finelli
Advances in genomic analyses based on next generation sequencing and integrated omics approaches, have accelerated in an unprecedented way the discovery of causative genes of developmental delay (DD) and intellectual disability (ID) disorders. Chromatin dysregulation has been recognized as common pathomechanism of mendelian DD/ID syndromes due to mutation in genes encoding chromatin regulators referred as transcriptomopathies or epigenetic disorders. Common to these syndromes are the wide phenotypic breadth and the recognition of groups of distinct syndromes with shared signs besides cognitive impairment, likely mirroring common molecular mechanisms...
April 19, 2018: Clinical Genetics
https://www.readbyqxmd.com/read/29671337/non-histone-targets-of-kat2a-and-kat2b-implicated-in-cancer-biology
#20
Emma Bondy-Chorney, Alix Denoncourt, Yuka Sai, Michael Downey
Lysine acetylation is a critical post-translation modification that can impact a protein's localization, stability and function. Originally thought to only occur on histones, we now know thousands of non-histone proteins are also acetylated. In conjunction with many other proteins, lysine acetyltransferases (KATs) are incorporated into large protein complexes that carry out these modifications. In this review we focus on the contribution of two KATs, KAT2A and KAT2B, and their potential roles in the development and progression of cancer...
April 19, 2018: Biochemistry and Cell Biology, Biochimie et Biologie Cellulaire
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