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HDAC1 HDAC2

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https://www.readbyqxmd.com/read/29096654/the-analgesic-effects-of-triptolide-in-the-bone-cancer-pain-rats-via-inhibiting-the-upregulation-of-hdacs-in-spinal-glial-cells
#1
Xiao-Fan Hu, Xiao-Tao He, Kai-Xiang Zhou, Chen Zhang, Wen-Jun Zhao, Ting Zhang, Jin-Lian Li, Jian-Ping Deng, Yu-Lin Dong
BACKGROUND: Bone cancer pain (BCP) severely compromises the quality of life, while current treatments are still unsatisfactory. Here, we tested the antinociceptive effects of triptolide (T10), a substance with considerable anti-tumor efficacies on BCP, and investigated the underlying mechanisms targeting the spinal dorsal horn (SDH). METHODS: Intratibial inoculation of Walker 256 mammary gland carcinoma cells was used to establish a BCP model in rats. T10 was intrathecally injected, and mechanical allodynia was tested by measuring the paw withdrawal thresholds (PWTs)...
November 2, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29080240/design-synthesis-molecular-modeling-and-biological-evaluation-of-novel-amine-based-histone-deacetylase-inhibitors
#2
Pavel A Petukhov, Hazem Abdelkarim, Raghupathi Neelarapu, Antonett Madriaga, Irida Kastrati, Yue-Ting Wang, Aditya S Vaidya, Taha Y Taha, Gregory R J Thatcher, Jonna Frasor
Histone deacetylases (HDACs) are promising drug targets for a variety of therapeutic applications. Here we describe the design, synthesis, biological evaluation in cellular models of cancer, and preliminary drug metabolism and pharmacokinetic studies (DMPK) of a series of secondary and tertiary amine-based HDAC inhibitors. Introduction of an amino group with one or two surface binding groups (SBGs) yielded a successful strategy to develop novel and potent HDAC inhibitors. Secondary amines 2 were found to be generally more potent than the corresponding tertiary amines 3...
October 27, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29050320/epigenetic-regulation-of-interleukin-8-expression-by-class-i-hdac-and-cbp-in-ovarian-cancer-cells
#3
Himavanth R Gatla, Yue Zou, Mohammad M Uddin, Ivana Vancurova
Although inhibitors of epigenetic regulators have been effective in the treatment of cutaneous T cell lymphoma (CTCL) and other hematopoietic malignancies, they have been less effective in solid tumors, including ovarian cancer (OC). We have previously shown that inhibition of histone deacetylase (HDAC) activity induces expression of the pro-inflammatory and pro-angiogenic chemokine interleukin-8 (CXCL8, IL-8) in OC cells, resulting in their increased survival and proliferation. Here, we show that in addition to ovarian cancer SKOV3, OVCAR3, and CAOV3 cells, HDAC inhibition induces the CXCL8 expression in HeLa cells, but not in CTCL Hut-78 cells...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29045501/scaffold-dependent-histone-deacetylase-hdac-inhibitor-induced-re-equilibration-of-the-subcellular-localization-and-post-translational-modification-state-of-class-i-hdacs
#4
Thomas W Hanigan, Taha Y Taha, Shaimaa M Aboukhatwa, Jonna Frasor, Pavel A Petukhov
The mechanism of action of histone deacetylase inhibitors (HDACi) is mainly attributed to the inhibition of the deacetylase catalytic activity for their histone substrates. In this study, we analyzed the abundance of class I HDACs in the cytosolic, nuclear soluble and chromatin bound cellular fractions in breast cancer cells after HDACi treatment. We found that potent N-hydroxy propenamide-based HDACi induced a concentration dependent decrease in the HDAC1 associated with chromatin and a lasting concomitant increase in cytoplasmic HDAC1 while maintaining total protein expression...
2017: PloS One
https://www.readbyqxmd.com/read/28987602/design-and-synthesis-of-tranylcypromine-derivatives-as-novel-lsd1-hdacs-dual-inhibitors-for-cancer-treatment
#5
Ying-Chao Duan, Yong-Cheng Ma, Wen-Ping Qin, Li-Na Ding, Yi-Chao Zheng, Ying-Li Zhu, Xiao-Yu Zhai, Jing Yang, Chao-Ya Ma, Yuan-Yuan Guan
Lysine specific demethylase 1 (LSD1) and Histone deacetylases (HDACs) are promising drug targets for cancers. Recent studies reveal an important functional interplay between LSD1 and HDACs, and there is evidence for the synergistic effect of combined LSD1 and HDAC inhibitors on cancers. Therefore, development of inhibitors targeting both LSD1 and HDACs might be a promising strategy for epigenetic therapy of cancers. We report herein the synthesis of a series of tranylcypromine derivatives as LSD1/HDACs dual inhibitors...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28982677/inhibiting-histone-deacetylase-2-hdac2-promotes-functional-recovery-from-stroke
#6
Ying Tang, Yu-Hui Lin, Huan-Yu Ni, Jian Dong, Hong-Jin Yuan, Yu Zhang, Hai-Ying Liang, Meng-Cheng Yao, Qi-Gang Zhou, Hai-Yin Wu, Lei Chang, Chun-Xia Luo, Dong-Ya Zhu
BACKGROUND: Stroke is a leading cause of long-term disability worldwide. However, current therapies that promote functional recovery from stroke are limited to physical rehabilitation. No pharmacological therapy is available. Thus, understanding the role of histone deacetylase 2 (HDAC2) in the pathophysiological process of stroke-induced functional loss may provide a novel strategy for stroke recovery. METHODS AND RESULTS: Focal stroke was induced by photothrombosis...
October 5, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28982113/crispr-mediated-hdac2-disruption-identifies-two-distinct-classes-of-target-genes-in-human-cells
#7
Priyanka Somanath, Rachel Herndon Klein, Paul S Knoepfler
The transcriptional functions of the class I histone deacetylases (HDACs) HDAC1 and HDAC2 are mainly viewed as both repressive and redundant based on murine knockout studies, but they may have additional independent roles and their physiological functions in human cells are not as clearly defined. To address the individual epigenomic functions of HDAC2, here we utilized CRISPR-Cas9 to disrupt HDAC2 in human cells. We find that while HDAC2 null cells exhibited signs of cross-regulation between HDAC1 and HDAC2, specific epigenomic phenotypes were still apparent using RNA-seq and ChIP assays...
2017: PloS One
https://www.readbyqxmd.com/read/28962688/hdac2-was-involved-in-placental-p-glycoprotein-regulation-both-in%C3%A2-vitro-and-vivo
#8
Hongyu Duan, Kaiyu Zhou, Yi Zhang, Peng Yue, Tao Wang, Yifei Li, Dajian Qiu, Jinlin Wu, Yimin Hua, Chuan Wang
INTRODUCTION: Placental P-glycoprotein (P-gp) plays a significant role in regulating drugs' transplacental transfer rates. Investigations on placental P-gp regulation could provide more therapeutic targets for individualized and safe pharmacotherapy during pregnancy. Currently, the epigenetic regulation of placental P-gp is rare. Our previous study has demonstrated that HDACs inhibition could up-regulate placental P-gp and HDAC1/2/3 might be involved in this process. The present study was carried out to further explore whether HDAC1/2/3 were indeed involved in the regulation of placental P-gp or not and screen out the subtype engaged in this process...
October 2017: Placenta
https://www.readbyqxmd.com/read/28959017/the-whhere-coactivator-complex-is-required-for-retinoic-acid-dependent-regulation-of-embryonic-symmetry
#9
Gonçalo C Vilhais-Neto, Marjorie Fournier, Jean-Luc Plassat, Mihaela E Sardiu, Anita Saraf, Jean-Marie Garnier, Mitsuji Maruhashi, Laurence Florens, Michael P Washburn, Olivier Pourquié
Bilateral symmetry is a striking feature of the vertebrate body plan organization. Vertebral precursors, called somites, provide one of the best illustrations of embryonic symmetry. Maintenance of somitogenesis symmetry requires retinoic acid (RA) and its coactivator Rere/Atrophin2. Here, using a proteomic approach we identify a protein complex, containing Wdr5, Hdac1, Hdac2 and Rere (named WHHERE), which regulates RA signaling and controls embryonic symmetry. We demonstrate that Wdr5, Hdac1, and Hdac2 are required for RA signaling in vitro and in vivo...
September 28, 2017: Nature Communications
https://www.readbyqxmd.com/read/28892521/a-systems-medicine-approach-for-finding-target-proteins-affecting-treatment-outcomes-in-patients-with-non-hodgkin-lymphoma
#10
Faezeh Ajorloo, Mohammad Vaezi, Alireza Saadat, Seyed Reza Safaee, Behrouz Gharib, Mostafa Ghanei, Seyed Davar Siadat, Farzam Vaziri, Abolfazl Fateh, Mehrdad Pazhouhandeh, Behrouz Vaziri, Reza Moazemi, Fereidoun Mahboudi, Fatemeh Rahimi Jamnani
Autoantibody profiling with a systems medicine approach can help identify critical dysregulated signaling pathways (SPs) in cancers. In this way, immunoglobulins G (IgG) purified from the serum samples of 92 healthy controls, 10 pre-treated (PR) non-Hodgkin lymphoma (NHL) patients, and 20 NHL patients who underwent chemotherapy (PS) were screened with a phage-displayed random peptide library. Protein-protein interaction networks of the PR and PS groups were analyzed and visualized by Gephi. The results indicated AXIN2, SENP2, TOP2A, FZD6, NLK, HDAC2, HDAC1, and EHMT2, in addition to CAMK2A, PLCG1, PLCG2, GRM5, GRIN2B, GRIN2D, CACNA2D3, and SPTAN1 as hubs in 11 and 7 modules of PR and PS networks, respectively...
2017: PloS One
https://www.readbyqxmd.com/read/28818449/rational-design-synthesis-and-preliminary-antitumor-activity-evaluation-of-a-chlorambucil-derivative-with-potent-dna-hdac-dual-targeting-inhibitory-activity
#11
Rui Xie, Yan Li, Pingwah Tang, Qipeng Yuan
Histone deacetylases (HDACs) play a pivotal role not only in gene expression but also in DNA repair. Herein, we report the successful design, synthesis and evaluation of a chlorambucil derivative named vorambucil with a hydroxamic acid tail as a DNA/HDAC dual-targeting inhibitor. Vorambucil obtained both potent DNA and HDACs inhibitory activities. Molecular docking results supported the initial pharmacophoric hypothesis and rationalized the potent inhibitory activity of vorambucil against HDAC1, HDAC2 and HDAC6...
September 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28796285/inhibition-of-histone-deacetylase-1-or-2-reduces-induced-cytokine-expression-in-microglia-through-a-protein-synthesis-independent-mechanism
#12
Benjamin S Durham, Ronald Grigg, Ian C Wood
Histone deacetylase (HDAC) inhibitors prevent neural cell death in in vivo models of cerebral ischaemia, brain injury and neurodegenerative disease. One mechanism by which HDAC inhibitors may do this is by suppressing the excessive inflammatory response of chronically activated microglia. However, the molecular mechanisms underlying this anti-inflammatory effect and the specific HDAC responsible are not fully understood. Recent data from in vivo rodent studies have shown that inhibition of class I HDACs suppresses neuroinflammation and is neuroprotective...
October 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28791750/histone-deacetylase-1-and-2-are-essential-for-murine-neural-crest-proliferation-pharyngeal-arch-development-and-craniofacial-morphogenesis
#13
Zachary J Milstone, Grace Lawson, Chinmay M Trivedi
BACKGROUND: Craniofacial anomalies involve defective pharyngeal arch development and neural crest function. Copy number variation at 1p35, containing histone deacetylase 1 (Hdac1), or 6q21-22, containing Hdac2, are implicated in patients with craniofacial defects, suggesting an important role in guiding neural crest development. However, the roles of Hdac1 and Hdac2 within neural crest cells remain unknown. RESULTS: The neural crest and its derivatives express both Hdac1 and Hdac2 during early murine development...
December 2017: Developmental Dynamics: An Official Publication of the American Association of Anatomists
https://www.readbyqxmd.com/read/28780164/changes-in-epigenetic-markers-dnmt1-and-hdac1-2-in-the-adult-mouse-hippocampus-after-cranial-irradiation
#14
Sohi Kang, Yeonghoon Son, Sueun Lee, Juhwan Kim, Jong-Choon Kim, Joong-Sun Kim, Uhee Jung, Sung-Ho Kim, Miyoung Yang, Changjong Moon
Brain exposure to ionizing radiation can cause functional deficits in the hippocampus, including memory impairment. However, the specific molecular mechanisms underlying irradiation-induced cognitive impairments are largely unknown. Changes in DNA methyltransferases (DNMTs) and histone deacetylases (HDACs), which are involved in DNA methylation and histone remodeling, may be associated with behavioral changes in learning and memory. We assessed changes in the levels of enzymes associated with the epigenetic modification of gene expression, including DNMT1, HDAC1, HDAC2, Sirtuin 1 (SIRT1), and acetylated histone H3 (Ace-H3) in the mouse hippocampus 1 and 30days after a single exposure to cranial irradiation (0 or 10Gy)...
September 14, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28776729/sirt1-activates-the-expression-of-fetal-hemoglobin-genes
#15
Yan Dai, Tyngwei Chen, Heba Ijaz, Elizabeth H Cho, Martin H Steinberg
High fetal hemoglobin (HbF, α2 γ2 ) levels ameliorate the clinical manifestations of sickle cell disease and β thalassemia. The mechanisms that repress HbF expression and silence γ-globin genes in adults are incompletely characterized and only a single HbF inducer, hydroxyurea, is approved for treatment, and only in patients with sickle cell disease. We identified SIRT1, a protein deacetylase, as a new inducer of γ-globin. SIRT1 knockdown decreased, while SIRT1 ectopic expression upregulated γ-globin gene (HBG) expression in primary human erythroid cells and in K562 cells...
November 2017: American Journal of Hematology
https://www.readbyqxmd.com/read/28769891/histone-deacetylase-2-is-a-component-of-influenza-a-virus-induced-host-antiviral-response
#16
Prashanth T Nagesh, Mazhar Hussain, Henry D Galvin, Matloob Husain
Host cells produce variety of antiviral factors that create an antiviral state and target various stages of influenza A virus (IAV) life cycle to inhibit infection. However, IAV has evolved various strategies to antagonize those antiviral factors. Recently, we reported that a member of class I host histone deacetylases (HDACs), HDAC1 possesses an anti-IAV function. Herein, we provide evidence that HDAC2, another class I member and closely related to HDAC1 in structure and function, also possesses anti-IAV properties...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28683591/the-ketone-metabolite-%C3%AE-hydroxybutyrate-attenuates-oxidative-stress-in-spinal-cord-injury-by-suppression-of-class-i-histone-deacetylases
#17
Ganggang Kong, Zucheng Huang, Wei Ji, Xiaomeng Wang, Junhao Liu, Xiuhua Wu, Zhiping Huang, Rong Li, Qingan Zhu
The ketone metabolite β-hydroxybutyrate (βOHB), is reported to be neuroprotective after spinal cord injury (SCI) in rats, but the underlying mechanism remains unknown. The present study aims to investigate effects of βOHB on suppression of oxidative stress and inhibition of class I histone deacetylases (HDACs) in in vivo and in vitro models. Rats were fed with ketogenic diet (KD) or standard diet (SD) for 3 weeks. A C5 hemi-contusion injury was applied to these animals on the 14th day of experiment, and spinal cord samples were harvested on the 1st, 3rd and 7th days after SCI, respectively...
September 15, 2017: Journal of Neurotrauma
https://www.readbyqxmd.com/read/28641467/green-tea-polyphenol-egcg-causes-anti-cancerous-epigenetic-modulations-in-acute-promyelocytic-leukemia-cells
#18
Veronika Borutinskaitė, Aida Virkšaitė, Giedrė Gudelytė, Rūta Navakauskienė
Green tea (Camellia sinensis) catechin epigallocatechin-3-gallate (EGCG) has been shown to possess diverse anti-cancerous properties. We demonstrated EGCG ability to inhibit acute promyelocytic leukemia (APL) cell proliferation and cause apoptosis. In addition, quantitative real-time polymerase chain reaction (RT-qPCR) analysis revealed elevated expression of genes associated with cell cycle arrest and differentiation (p27, PCAF, C/EBPα, and C/EBPɛ). Furthermore, EGCG caused anti-cancerous epigenetic changes: downregulation of epigenetic modifiers DNMT1, HDAC1, HDAC2, and G9a was observed by RT-qPCR analysis...
June 22, 2017: Leukemia & Lymphoma
https://www.readbyqxmd.com/read/28629630/design-synthesis-and-tumor-cell-growth-inhibitory-activity-of-3-nitro-2h-cheromene-derivatives-as-histone-deacetylaes-inhibitors
#19
Shuai Tan, Feng He, Tingting Kong, Jingde Wu, Zhaopeng Liu
As a continuous research for the discovery of coumarin-based targeted anticancer agents, we designed and synthesized a series of novel histone deacetylases (HDAC) inhibitors using the 8-ethoxy-3-nitro-2H-chromene as the surface binding or cap group, linear dicarboxylic acid or ω-amino acid moiety with different length as the linking motif, ortho-aminoanilides, amides or α-aminoamides as the zinc binding group and the internal cavity motifs. Most of these 3-nitro-2H-chromene derivatives exhibited good growth inhibitory activity against K562, A549, MCF-7, PC3 and Hela cells and were more potent than the reference drug SAHA and MS-275...
June 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28628607/host-gene-expression-analysis-in-sri-lankan-melioidosis-patients
#20
Shivankari Krishnananthasivam, Nimanthi Jayathilaka, Harindra Darshana Sathkumara, Enoka Corea, Mohan Natesan, Aruna Dharshan De Silva
BACKGROUND: Melioidosis is a life threatening infectious disease caused by the gram-negative bacillus Burkholderia pseudomallei predominantly found in southeast Asia and northern Australia. Studying the host transcription profiles in response to infection is crucial for understanding disease pathogenesis and correlates of disease severity, which may help improve therapeutic intervention and survival. The aim of this study was to analyze gene expression levels of human host factors in melioidosis patients and establish useful correlation with disease biomarkers, compared to healthy individuals and patients with sepsis caused by other pathogens...
June 2017: PLoS Neglected Tropical Diseases
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