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https://www.readbyqxmd.com/read/28529458/targeting-hsp90-hdac6-regulating-network-implicates-precision-treatment-of-breast-cancer
#1
Shiyi Yu, Xiuxiu Cai, Chenxi Wu, Yan Liu, Jun Zhang, Xue Gong, Xin Wang, Xiaoli Wu, Tao Zhu, Lin Mo, Jun Gu, Zhenghong Yu, Jinfei Chen, Jean Paul Thiery, Renjie Chai, Liming Chen
Breast cancer is the leading cause of women death. Heat shock protein 90 (HSP90) and Histone deacetylase 6 (HDAC6) are promising anti-cancer drug targets. However, it's still unclear the applicability of anti-HSP90 and anti-HDAC6 strategies in precision treatment of breast cancer. In current study, we found that triple negative breast cancer (TNBC) cells, compared to T47D, an ERα+ breast cancer cell line, exhibited 7~40 times lower IC50 values, stronger cell cycle perturbation, increased cell apoptosis and stronger inhibition of cell migration upon 17-DMAG treatment, while T47D, compared to TNBC cells, expressed higher HDAC6 and showed stronger anti-cancer response upon treatment of Tubacin...
2017: International Journal of Biological Sciences
https://www.readbyqxmd.com/read/28523102/design-and-synthesis-of-mercaptoacetamides-as-potent-selective-and-brain-permeable-histone-deacetylase-6-inhibitors
#2
Wei Lv, Guangming Zhang, Cyril Barinka, James H Eubanks, Alan P Kozikowski
A series of nonhydroxamate HDAC6 inhibitors were prepared in our effort to develop potent and selective compounds for possible use in central nervous system (CNS) disorders, thus obviating the genotoxicity often associated with the hydroxamates. Halogens are incorporated in the cap groups of the designed mercaptoacetamides in order to increase brain accessibility. The indole analogue 7e and quinoline analogue 13a displayed potent HDAC6 inhibitory activity (IC50, 11 and 2.8 nM) and excellent selectivity against HDAC1...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28507509/loss-of-elp3-impairs-the-acetylation-and-distribution-of-connexin-43-in-the-developing-cerebral-cortex
#3
Sophie Laguesse, Pierre Close, Laura Van Hees, Alain Chariot, Brigitte Malgrange, Laurent Nguyen
The Elongator complex is required for proper development of the cerebral cortex. Interfering with its activity in vivo delays the migration of postmitotic projection neurons, at least through a defective α-tubulin acetylation. However, this complex is already expressed by cortical progenitors where it may regulate the early steps of migration by targeting additional proteins. Here we report that connexin-43 (Cx43), which is strongly expressed by cortical progenitors and whose depletion impairs projection neuron migration, requires Elongator expression for its proper acetylation...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28499252/crosstalk-between-hdac6-and-nox2-based-nadph-oxidase-mediates-hiv-1-tat-induced-pro-inflammatory-responses-in-astrocytes
#4
Gi Soo Youn, Hyundong Cho, Donggyu Kim, Soo Young Choi, Jinseu Park
Histone deacetylase 6 (HDAC6) likely is important in inflammatory diseases. However, how HDAC6 exerts its effect on inflammatory processes remains unclear. HIV-1 transactivator of transcription (Tat) activates NADPH oxidase resulting in generation of reactive oxygen species (ROS), leading to extensive neuro-inflammation in the central nervous system. We investigated the correlation of HDAC6 and NADPH oxidase in HIV-1 Tat-stimulated astrocytes. HDAC6 knockdown attenuated HIV-1 Tat-induced ROS generation and NADPH oxidase activation...
May 4, 2017: Redox Biology
https://www.readbyqxmd.com/read/28496307/developing-selective-histone-deacetylases-hdacs-inhibitors-through-ebselen-and-analogs
#5
Yuren Wang, Jason Wallach, Stephanie Duane, Yuan Wang, Jianghong Wu, Jeffrey Wang, Adeboye Adejare, Haiching Ma
Histone deacetylases (HDACs) are key regulators of gene expression in cells and have been investigated as important therapeutic targets for cancer and other diseases. Different subtypes of HDACs appear to play disparate roles in the cells and are associated with specific diseases. Therefore, substantial effort has been made to develop subtype-selective HDAC inhibitors. In an effort to discover existing scaffolds with HDAC inhibitory activity, we screened a drug library approved by the US Food and Drug Administration and a National Institutes of Health Clinical Collection compound library in HDAC enzymatic assays...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28491824/rabies-virus-infection-induces-microtubule-depolymerization-to-facilitate-viral-rna-synthesis-by-upregulating-hdac6
#6
Jie Zan, Song Liu, Dong-Nan Sun, Kai-Kun Mo, Yan Yan, Juan Liu, Bo-Li Hu, Jin-Yan Gu, Min Liao, Ji-Yong Zhou
Rabies virus (RABV) is the cause of rabies, and is associated with severe neurological symptoms, high mortality rate, and a serious threat to human health. Although cellular tubulin has recently been identified to be incorporated into RABV particles, the effects of RABV infection on the microtubule cytoskeleton remain poorly understood. In this study, we show that RABV infection induces microtubule depolymerization as observed by confocal microscopy, which is closely associated with the formation of the filamentous network of the RABV M protein...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28471062/pharmacologically-increasing-microtubule-acetylation-corrects-stress-exacerbated-effects-of-organophosphates-on-neurons
#7
Anand N Rao, Ankita Patil, Zachary D Brodnik, Liang Qiang, Rodrigo A Espana, Kimberly A Sullivan, Mark M Black, Peter W Baas
Many veterans of the 1990-1991 Gulf War contracted Gulf War Illness, a multi-symptom disease that primarily affects the nervous system. Here we treated cultures of human or rat neurons with diisopropylfluorophosphate (DFP), an analog of sarin, one of the organophosphate toxicants to which the military veterans were exposed. All observed cellular defects produced by DFP were exacerbated by pretreatment with corticosterone or cortisol, which, in the rat and human neurons respectively, serves in our experiments to mimic the physical stress endured by soldiers during the war...
May 4, 2017: Traffic
https://www.readbyqxmd.com/read/28468311/tubacin-an-hdac6-selective-inhibitor-reduces-the-replication-of-the-japanese-encephalitis-virus-via-the-decrease-of-viral-rna-synthesis
#8
Chien-Yi Lu, Yi-Chih Chang, Chun-Hung Hua, Chieh Chuang, Su-Hua Huang, Szu-Hao Kung, Mann-Jen Hour, Cheng-Wen Lin
Japanese encephalitis virus (JEV), a neurotropic flavivirus, annually causes over 30,000 Japanese Encephalitis (JE) cases in East and Southeast Asia. Histone deacetylases (HDACs) modulate lysine acetylation of histones and non-histone proteins, regulating many processes including inflammation and antiviral immune response. This study investigated antiviral activity of pan- and selective-HDAC inhibitors as host-targeting agents against JEV. Among HDAC inhibitors, selective HDAC6 inhibitors (tubastatin-A (TBSA) and tubacin) concentration-dependently inhibited JEV-induced cytopathic effect and apoptosis, as well as reduced virus yield in human cerebellar medulloblastoma cells...
May 1, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28453994/synthesis-and-applications-of-benzohydroxamic-acid-based-histone-deacetylase-inhibitors
#9
REVIEW
Rob De Vreese, Matthias D'hooghe
This paper provides an overview of the synthesis and biological activity of the most representative benzohydroxamic acid-based histone deacetylase inhibitors published to date. Benzohydroxamic acids comprise an important class of HDAC inhibitors, and recently several of these structures have been evaluated in clinical trials for the treatment of a variety of cancers. In this overview, benzohydroxamic acids were divided in four different classes based on their reported selectivity towards zinc-dependent HDACs: a first and major class consists of HDAC6 selective inhibitors, a second class deals with pan-HDAC inhibitors, a third class comprises HDAC8 selective inhibitors and a fourth, minor class includes dual HDAC6/8 selective inhibitors...
April 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28452069/the-hdac6-inhibitor-tubacin-induces-release-of-cd133-extracellular-vesicles-from-cancer-cells
#10
Olivia S Chao, Tim C Chang, Maria A Di Bella, Riccardo Alessandro, Fabio Anzanello, Germana Rappa, Oscar B Goodman, Aurelio Lorico
Tumor-derived extracellular vesicles (EVs) are emerging as an important mode of intercellular communication, capable of transferring biologically active molecules that facilitate the malignant growth and metastatic process. CD133 (Prominin-1), a stem cell marker implicated in tumor initiation, differentiation and resistance to anti-cancer therapy, is reportedly associated with EVs in various types of cancer. However, little is known about the factors that regulate the release of these CD133(+) EVs. Here, we report that the HDAC6 inhibitor tubacin promoted the extracellular release of CD133(+) EVs from human FEMX-I metastatic melanoma and Caco-2 colorectal carcinoma cells, with a concomitant downregulation of intracellular CD133...
April 27, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28437526/prominin-1-is-a-novel-regulator-of-autophagy-in-the-human-retinal-pigment-epithelium
#11
Sujoy Bhattacharya, Jinggang Yin, Christina S Winborn, Qiuhua Zhang, Junming Yue, Edward Chaum
Purpose: Prominin-1 (Prom1) is a transmembrane glycoprotein, which is expressed in stem cell lineages, and has recently been implicated in cancer stem cell survival. Mutations in the Prom1 gene have been shown to disrupt photoreceptor disk morphogenesis and cause an autosomal dominant form of Stargardt-like macular dystrophy (STGD4). Despite the apparent structural role of Prom1 in photoreceptors, its role in other cells of the retina is unknown. The purpose of this study is to investigate the role of Prom1 in the highly metabolically active cells of the retinal pigment epithelium (RPE)...
April 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28424080/erratum-to-hdac6-activity-is-a-non-oncogene-addiction-hub-for-inflammatory-breast-cancers
#12
Preeti Putcha, Jiyang Yu, Ruth Rodriguez-Barrueco, Laura Saucedo-Cuevas, Patricia Villagrasa, Eva Murga-Penas, Steven N Quayle, Min Yang, Veronica Castro, David Llobet-Navas, Daniel Birnbaum, Pascal Finetti, Wendy A Woodward, François Bertucci, Mary L Alpaugh, Andrea Califano, Jose Silva
No abstract text is available yet for this article.
April 19, 2017: Breast Cancer Research: BCR
https://www.readbyqxmd.com/read/28419930/design-synthesis-and-anticancer-potential-of-nsc-319745-hydroxamic-acid-derivatives-as-dnmt-and-hdac-inhibitors
#13
Zigao Yuan, Qinsheng Sun, Dan Li, Shuangshuang Miao, Shaopeng Chen, Lu Song, Chunmei Gao, Yuzong Chen, Chunyan Tan, Yuyang Jiang
DNA methyltransferases (DNMTs) and histone deacetylases (HDACs) are important epigenetic targets during anticancer drug development. Recent study indicates that DNMT inhibitors and HDAC inhibitors display synergistic effects in certain cancers, therefore, development of molecules targeting both DNMT and HDAC is of therapeutic advantage against these cancers. Based on the structure of DNMT inhibitor NSC-319745 and the pharmacophore characteristics of HDAC inhibitors, a series of hydroxamic acid derivatives of NSC-319745 were designed and synthesized as DNMT and HDAC multifunctional inhibitors...
April 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28408401/synergistic-immunostimulatory-effects-and-therapeutic-benefit-of-combined-histone-deacetylase-and-bromodomain-inhibition-in-non-small-cell-lung-cancer
#14
Dennis Adeegbe, Yan Liu, Patrick H Lizotte, Yusuke Kamihara, Amir R Aref, Christina Almonte, Ruben Dries, Yuyang Li, Shengwu Liu, Xiaoen Wang, Tiquella Warner-Hatten, Jessica Castrillon, Guo-Cheng Yuan, Neermala Poudel-Neupane, Haikuo Zhang, Jennifer L Guerriero, Shiwei Han, Mark M Awad, David A Barbie, Jerome Ritz, Simon S Jones, Peter S Hammerman, James E Bradner, Steven N Quayle, Kwok-Kin Wong
Effective therapies for non-small cell lung cancer (NSCLC) remain challenging despite an increasingly comprehensive understanding of somatically altered oncogenic pathways. It is now clear that therapeutic agents with potential to impact the tumor immune microenvironment potentiate immune-orchestrated therapeutic benefit. Herein we evaluated the immunoregulatory properties of histone deacetylase (HDAC) and bromodomain inhibitors, two classes of drugs that modulate the epigenome, with a focus on key cell subsets that are engaged in an immune response...
April 13, 2017: Cancer Discovery
https://www.readbyqxmd.com/read/28398261/novel-proteasome-inhibitors-and-histone-deacetylase-inhibitors-progress-in-myeloma-therapeutics
#15
REVIEW
Saurabh Chhabra
The unfolded protein response is responsible for the detection of misfolded proteins and the coordination of their disposal and is necessary to maintain the cellular homoeostasis. Multiple myeloma cells secrete large amounts of immunoglobulins, proteins that need to be correctly folded by the chaperone system. If this process fails, the misfolded proteins have to be eliminated by the two main garbage-disposal systems of the cell: proteasome and aggresome. The blockade of either of these systems will result in accumulation of immunoglobulins and other toxic proteins in the cytoplasm and cell death...
April 11, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28382171/hdac6-regulates-il-17-expression-in-t-lymphocytes-implications-for-hdac6-targeted-therapies
#16
Bing Yan, Yang Liu, Hong Bai, Miao Chen, Songbo Xie, Dengwen Li, Min Liu, Jun Zhou
The pro-inflammatory cytokine interleukin 17 (IL-17) is critically involved in immunity and inflammation. T-helper 17 and γδ T cells are the predominant sources of IL-17 in the immune system. However, the mechanisms by which the expression of IL-17 is regulated in T cells remain elusive. Here, we demonstrate that loss of histone deacetylase 6 (HDAC6) in mice does not affect the generation of CD4(+) or CD8(+) T cells, but stimulates the development of IL-17-producing γδ T cells. Our data further show that HDAC6 deficiency increases the production of IL-17 by Vγ4(+) γδ T cells in the spleen and lymph nodes...
2017: Theranostics
https://www.readbyqxmd.com/read/28374847/effect-of-agomelatine-on-memory-deficits-and-hippocampal-gene-expression-induced-by-chronic-social-defeat-stress-in-mice
#17
Vincent Martin, Najib Allaïli, Marine Euvrard, Tevrasamy Marday, Armance Riffaud, Bernard Franc, Elisabeth Mocaër, Cecilia Gabriel, Philippe Fossati, Stéphane Lehericy, Laurence Lanfumey
Chronic stress is known to induce not only anxiety and depressive-like phenotypes in mice but also cognitive impairments, for which the action of classical antidepressant compounds remains unsatisfactory. In this context, we investigated the effects of chronic social defeat stress (CSDS) on anxiety-, social- and cognitive-related behaviors, as well as hippocampal Bdnf, synaptic plasticity markers (PSD-95, Synaptophysin, Spinophilin, Synapsin I and MAP-2), and epigenetic modifying enzymes (MYST2, HDAC2, HDAC6, MLL3, KDM5B, DNMT3B, GADD45B) gene expression in C57BL/6J mice...
April 4, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28342984/hdac4-and-hdac6-sustain-dna-double-strand-break-repair-and-stem-like-phenotype-by-promoting-radioresistance-in-glioblastoma-cells
#18
Francesco Marampon, Francesca Megiorni, Simona Camero, Clara Crescioli, Heather P McDowell, Roberta Sferra, Antonella Vetuschi, Simona Pompili, Luca Ventura, Francesca De Felice, Vincenzo Tombolini, Carlo Dominici, Roberto Maggio, Claudio Festuccia, Giovanni Luca Gravina
The role of histone deacetylase (HDAC) 4 and 6 in glioblastoma (GBM) radioresistance was investigated. We found that tumor samples from 31 GBM patients, who underwent temozolomide and radiotherapy combined treatment, showed HDAC4 and HDAC6 expression in 93.5% and 96.7% of cases, respectively. Retrospective clinical data analysis demonstrated that high-intensity HDAC4 and/or HDAC6 immunostaining was predictive of poor clinical outcome. In vitro experiments revealed that short hairpin RNA-mediated silencing of HDAC4 or HDAC6 radiosensitized U87MG and U251MG GBM cell lines by promoting DNA double-strand break (DSBs) accumulation and by affecting DSBs repair molecular machinery...
March 23, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28337317/structural-requirements-of-hdac-inhibitors-saha-analogues-modified-at-the-c2-position-display-hdac6-8-selectivity
#19
Ahmed T Negmeldin, Geetha Padige, Anton V Bieliauskas, Mary Kay H Pflum
Histone deacetylase (HDAC) proteins are epigenetic regulators that deacetylate protein substrates, leading to subsequent changes in cell function. HDAC proteins are implicated in cancers, and several HDAC inhibitors have been approved by the FDA as anticancer drugs, including SAHA (suberoylanilide hydroxamic acid; Vorinostat and Zolinza). Unfortunately, SAHA inhibits most HDAC isoforms, which limits its use as a pharmacological tool and may lead to side effects in the clinic. In this work SAHA analogues substituted at the C2 position were synthesized and screened for HDAC isoform selectivity in vitro and in cells...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28332438/quantitative-structure-activity-relationship-analysis-and-virtual-screening-studies-for-identifying-hdac2-inhibitors-from-known-hdac-bioactive-chemical-libraries
#20
H Pham-The, G Casañola-Martin, K Diéguez-Santana, N Nguyen-Hai, N T Ngoc, L Vu-Duc, H Le-Thi-Thu
Histone deacetylases (HDAC) are emerging as promising targets in cancer, neuronal diseases and immune disorders. Computational modelling approaches have been widely applied for the virtual screening and rational design of novel HDAC inhibitors. In this study, different machine learning (ML) techniques were applied for the development of models that accurately discriminate HDAC2 inhibitors form non-inhibitors. The obtained models showed encouraging results, with the global accuracy in the external set ranging from 0...
March 2017: SAR and QSAR in Environmental Research
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