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https://www.readbyqxmd.com/read/29142410/methanolic-extract-of-costus-pictus-d-don-induces-cytotoxicity-in-liver-hepatocellular-carcinoma-cells-mediated-by-histone-deacetylase-inhibition
#1
P V Neethu, K Suthindhiran, M A Jayasri
Background: Leaves of Costus pictus D. Don, (insulin plant) are used as dietary supplement for the treatment of diabetes. Objective: The antidiabetic activity of this plant is well documented, but its activity on different cell types and mechanism remains unknown. Thus, the present study evaluates the cytotoxicity of C. pictus methanolic extract (CPME) against various cancer and normal cells. Materials and Methods: Dried leaves of C. pictus were extracted using methanol and were subjected to histone deacetylase (HDAC) inhibition and toxicity studies...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29141538/curcumin-a-natural-pan-hdac-inhibitor-in-cancer
#2
Sara Saffar Soflaei, Amir Abbas Momtazi, Muhammed Majeed, Giuseppe Derosa, Pamela Maffioli, Amirhossein Sahebkar
BACKGROUND: Histone deacetylases (HDACs) are a group of histone modification enzymes with pivotal role in disease pathogenesis especially in cancer development. Increased activity of certain types of HDACs and positive effects of HDAC inhibition has been shown in several types of cancers. Furthermore, few HDAC inhibitors have been approved by the FDA for cancer treatment, and this has generated interest in finding new HDAC inhibitors as potential anti-cancer agents. Curcumin, a natural polyphenol extracted from turmeric, is a safe and bioactive phytochemical with a wide range of molecular targets and pharmacological activities including promising anti-cancer properties...
November 14, 2017: Current Pharmaceutical Design
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
#3
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/29072756/perfluorinated-hdac-inhibitors-as-selective-anticancer-agents
#4
James W Walton, Jasmine M Cross, Tina Riedel, Paul J Dyson
A series of potent histone deacetylase inhibitors is presented that incorporate alkyl or perfluorinated alkyl chains. Several new compounds show greater in vitro antiproliferative activity than the clinically approved inhibitor, SAHA. Furthermore, the new compounds show up to 5-fold greater activity against cancer cells than healthy cells. This selectivity is in contrast to SAHA, which is more active against the healthy cell line than the cancer cell line tested. Finally, we report an increase in activity for SAHA under mild hyperthermia, indicating that it could be an interesting candidate to use in combination with thermal therapy...
November 7, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29054638/the-persistent-organochlorine-pesticide-endosulfan-modulates-multiple-epigenetic-regulators-with-oncogenic-potential-in-mcf-7-cells
#5
Krishna Ghosh, Biji Chatterjee, Aparna Geetha Jayaprasad, Santosh R Kanade
Environmental cues and chemicals can potentially modulate the phenotypic expression of genome through alterations in the epigenetic mechanisms. Endosulfan is one of the extensively used organochlorine pesticides around the world which is known for its endocrine, neuro- and reproductive toxicity. This study was aimed to investigate the potential of α-endosulfan in modulation of multiple epigenetic enzymes in MCF-7 cells. The cells were treated with DMSO (control) or α-endosulfan (1 and 10μM) and the expression of various epigenetic enzymes was assayed by real-time PCR and immunoblotting, in addition to their activity assays...
October 17, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28966246/synergistic-inhibition-of-breast-cancer-cell-growth-by-an-epigenome-targeting-drug-and-a-tyrosine-kinase-inhibitor
#6
Yu Shan Wu, Yuan Quan, Dong Xing Zhang, Dong Wu Liu, Xiu Zhen Zhang
BACKGROUND: Epigenome-targeting drugs, for example, histone decetylases (HDACs) inhibitors, have been recently shown to induce apoptosis in a variety of cancer cells, which could potentially be used as anticancer therapy. Tyrosine kinase inhibitors (TKIs) have been widely used in clinical trials of various cancers. HDAC inhibitor vorinostat, TKIs dasatinib have been tested in pivotal phase 2 clinical trials in patients with breast cancer. The combination treatment of vorinostat with dasatinib is expected to have synergistic effect on inhibiting breast cancer cell growth...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28962688/hdac2-was-involved-in-placental-p-glycoprotein-regulation-both-in%C3%A2-vitro-and-vivo
#7
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/28958182/epigenetic-changes-in-the-early-stage-of-silica-induced-cell-transformation
#8
Carole Seidel, Anaïs Kirsch, Caroline Fontana, Athanase Visvikis, Aurélie Remy, Laurent Gaté, Christian Darne, Yves Guichard
The increasing use of nanomaterials in numerous domains has led to growing concern about their potential toxicological properties, and the potential risk to human health posed by silica nanoparticles remains under debate. Recent studies proposed that these particles could alter gene expression through the modulation of epigenetic marks, and the possible relationship between particle exposure and these mechanisms could represent a critical factor in carcinogenicity. In this study, using the Bhas 42 cell model, we compare the effects of exposure to two transforming particles, a pyrogenic amorphous silica nanoparticle NM-203 to those of the crystalline silica particle Min-U-Sil(®) 5...
September 28, 2017: Nanotoxicology
https://www.readbyqxmd.com/read/28954936/different-schedule-dependent-effects-of-epigenetic-modifiers-on-cytotoxicity-by-anticancer-drugs-in-colorectal-cancer-cells
#9
Mika Hosokawa, Shota Tanaka, Kumiko Ueda, Seigo Iwakawa
Limited information is currently available on how to apply epigenetic modifiers to current colorectal cancer (CRC) chemotherapy. The purpose of this study is to clarify the schedule-dependent effects of combined treatment with conventional anticancer drugs and epigenetic modifiers in human CRC cells. Cytotoxicity in 4 CRC cell lines (SW480, HT29, SW48, and HCT116) was measured using the WST-8 assay. As epigenetic modifiers, 3 DNA methyltransferase (DNMT) inhibitors such as decitabine (DAC), azacytidine (AC), and zebularine (Zeb), and 3 histone deacetylase (HDAC) inhibitors including trichostatin A (TSA), suberoylanilide hydroxamic acid (SAHA), and valproic acid (VPA) were used...
September 28, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28953929/class-ii-and-iv-hdacs-function-as-inhibitors-of-osteoclast-differentiation
#10
Nicholas C Blixt, Bora K Faulkner, Kristina Astleford, Rosemary Lelich, Jacob Schering, Ekaterina Spencer, Rajaram Gopalakrishnan, Eric D Jensen, Kim C Mansky
Histone deacetylases (HDACs) are negative regulators of transcription and have been shown to regulate specific changes in gene expression. In vertebrates, eighteen HDACs have thus far been identified and subdivided into four classes (I-IV). Key roles for several HDACs in bone development and biology have been elucidated through in vitro and in vivo models. By comparison, there is a paucity of data on the roles of individual HDACs in osteoclast formation and function. In this study, we investigated the gene expression patterns and the effects of suppressing individual class II (Hdac4, 5, 6, 9, and 10) and class IV (Hdac11) HDACs during osteoclast differentiation...
2017: PloS One
https://www.readbyqxmd.com/read/28948877/insights-into-intermolecular-interactions-electrostatic-properties-and-the-stability-of-c646-in-the-binding-pocket-of-p300-histone-acetyltransferase-enzyme-a-combined-molecular-dynamics-and-charge-density-study
#11
Sivanandam Magudeeswaran, Saravanan Kandasamy, Kumaradhas Poomani
Histone acetyltransferases (HATs) and Histone deacetylases (HDACs) are enzymes exhibit important transcription activity. Dysfunction of these enzymes may lead to different diseases including cancer, cardiovascular and other diseases. Therefore, these enzymes are the potential target for the generation of new therapeutics. C646 is a synthetic p300 HAT inhibitor, its structural and the electrostatic properties are the paradigm to understand its activity in the active site of p300 HAT enzyme. The docked C646 molecule in the active site forms expected key intermolecular interactions with the amino acid residues Trp1436, Tyr1467 and one water molecule (W1861); and these interactions are important for acetylation reaction...
September 26, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28943357/divergent-jnk-phosphorylation-of-hdac3-in-triple-negative-breast-cancer-cells-determines-hdac-inhibitor-binding-and-selectivity
#12
Thomas W Hanigan, Shaimaa M Aboukhatwa, Taha Y Taha, Jonna Frasor, Pavel A Petukhov
Histone deacetylase (HDAC) catalytic activity is regulated by formation of co-regulator complexes and post-translational modification. Whether these mechanisms are transformed in cancer and how this affects the binding and selectivity of HDAC inhibitors (HDACis) is unclear. In this study, we developed a method that identified a 3- to 16-fold increase in HDACi selectivity for HDAC3 in triple-negative breast cancer (TNBC) cells in comparison with luminal subtypes that was not predicted by current practice measurements with recombinant proteins...
November 16, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28939740/immunomodulation-by-entinostat-in-renal-cell-carcinoma-patients-receiving-high-dose-interleukin-2-a-multicenter-single-arm-phase-1-2-trial-nci-ctep-7870
#13
Roberto Pili, David I Quinn, Hans Hammers, J Paul Monk, Saby George, Tanya Dorff, Thomas Olencki, Li Shen, Ashley R Orillion, Dominick Lamonica, Roberto A Salas Fragomeni, Zsolt Szabo, Alan D Hutson, Adrienne Groman, Susan M Perkins, Richard L Piekarz, Michael A Carducci
PURPOSE: Based on preclinical data suggesting that the class I selective HDAC inhibitor entinostat exerts a synergistic antitumor effect in combination with high dose interleukin 2 (IL-2) in a renal cell carcinoma model by down-regulating Foxp3 expression and function of regulatory T cells (Treg), we conducted a phase I/II clinical study with entinostat and high dose IL-2 in patients with metastatic clear cell renal cell carcinoma (ccRCC). EXPERIMENTAL DESIGN: Clear cell histology, no prior treatments, and being sufficiently fit to receive high dose IL-2 were the main eligibility criteria...
September 22, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28918353/antitumor-platinum-iv-derivatives-of-carboplatin-and-the-histone-deacetylase-inhibitor-4-phenylbutyric-acid
#14
Awatif Rashed Z Almotairy, Valentina Gandin, Liam Morrison, Cristina Marzano, Diego Montagner, Andrea Erxleben
Five new platinum(IV) derivatives of carboplatin each incorporating the histone deacetylase inhibitor 4-phenylbutyrate in axial position were synthesized and characterized by (1)H and (195)Pt NMR spectroscopy, electrospray ionization mass spectrometry and elemental analysis, namely cis,trans-[Pt(CBDCA)(NH3)2(PBA)(OH)] (1), cis,trans-[Pt(CBDCA)(NH3)2(PBA)2] (2), cis,trans-[Pt(CBDCA)(NH3)2(PBA)(bz)] (3), cis,trans-[Pt(CBDCA)(NH3)2(PBA)(suc)] (4) and cis,trans-[Pt(CBDCA)(NH3)2)(PBA)(ac)] (5) (PBA=4-phenylbutyrate, CBDCA=1,1-cyclobutane dicarboxylate, bz=benzoate, suc=succinate and ac=acetate)...
September 10, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28916629/histone-deacetylase-inhibition-induces-odor-preference-memory-extension-and-maintains-enhanced-ampa-receptor-expression-in-the-rat-pup-model
#15
Sriya Bhattacharya, Bandhan Mukherjee, Jules J E Doré, Qi Yuan, Carolyn W Harley, John H McLean
Histone deacetylase (HDAC) plays a role in synaptic plasticity and long-term memory formation. We hypothesized that trichostatin-A (TSA), an HDAC inhibitor, would promote long-term odor preference memory and maintain enhanced GluA1 receptor levels that have been hypothesized to support memory. We used an early odor preference learning model in neonate rat pups that normally produces only 24-h memory to test behavior and examine receptor protein expression. Our behavioral studies showed that intrabulbar infusion of TSA, prior to pairing of the conditioned stimulus (peppermint odor) with the unconditioned stimulus (tactile stimulation), prolonged 24-h odor preference memory for at least 9 d...
October 2017: Learning & Memory
https://www.readbyqxmd.com/read/28915585/time-dependent-modulation-of-tumor-radiosensitivity-by-a-pan-hdac-inhibitor-abexinostat
#16
Sofia Rivera, Céline Leteur, Frédérique Mégnin, Frédéric Law, Isabelle Martins, Ioana Kloos, Stéphane Depil, Nazanine Modjtahedi, Jean Luc Perfettini, Christophe Hennequin, Eric Deutsch
Despite prominent role of radiotherapy in lung cancer management, there is an urgent need for strategies increasing therapeutic efficacy. Reversible epigenetic changes are promising targets for combination strategies using HDAC inhibitors (HDACi). Here we evaluated on two NSCLC cell lines, the antitumor effect of abexinostat, a novel pan HDACi combined with irradiation in vitro in normoxia and hypoxia, by clonogenic assays, demonstrating that abexinostat enhances radiosensitivity in a time dependent way with mean SER10 between 1...
August 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28883618/cg200745-an-hdac-inhibitor-induces-anti-tumour-effects-in-cholangiocarcinoma-cell-lines-via-mirnas-targeting-the-hippo-pathway
#17
Dawoon E Jung, Soo Been Park, Kahee Kim, Chanyang Kim, Si Young Song
Cholangiocarcinoma is a devastating malignancy with fatal complications that exhibits low response and resistance to chemotherapy. Here, we evaluated the anticancer effects of CG200745, a novel histone deacetylase inhibitor, either alone or in combination with standard chemotherapy drugs in cholangiocarcinoma cells. CG200745 dose-dependently reduced the viability of cholangiocarcinoma cells in vitro and decreased tumour volume and weight in a xenograft model. Administering CG200745 along with other chemotherapeutic agents including gemcitabine, 5-fluorouracil (5-FU), cisplatin, oxaliplatin, or gemcitabine plus cisplatin further decreased cholangiocarcinoma cell viability, with a combination index < 1 that indicated synergistic action...
September 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28860342/cudc-907-in-relapsed-refractory-diffuse-large-b-cell-lymphoma-including-patients-with-myc-alterations-results-from-an-expanded-phase-i-trial
#18
Yasuhiro Oki, Kevin R Kelly, Ian Flinn, Manish R Patel, Robert Gharavi, Anna Ma, Jefferson Parker, Amir Hafeez, David Tuck, Anas Younes
CUDC-907 is a first-in-class, oral small molecule inhibitor of both HDAC (class I and II) and PI3K (class Iα, β, and δ) enzymes, with demonstrated anti-tumor activity in multiple pre-clinical models, including MYC-driven ones. In this report, we present the safety and preliminary activity results of CUDC-907, with and without rituximab, in patients with relapsed/refractory diffuse large B-cell lymphoma (DLBCL), with a particular focus on those with MYC-altered disease. Thirty-seven DLBCL patients were enrolled, 14 with confirmed MYC-altered disease...
November 2017: Haematologica
https://www.readbyqxmd.com/read/28855102/age-related-alterations-in-histone-deacetylase-expression-in-purkinje-neurons-of-ethanol-fed-rats
#19
Abhilasha Khurana, Cynthia A Dlugos
Ethanol and age-induced pathologies of the Purkinje neuron (PN) may result from histone deacetylases (HDACs), enzymes which repress transcription through coiling of the DNA. The purposes of this study were to investigate expression patterns of Class 1 and IIa HDACs in PN and the effects of aging and alcohol on the density of HDACs and histone acetylation in PN. Ninety, eight month old rats (30/diet) were fed a liquid ethanol, liquid control, or rat chow diet for 10, 20, or 40weeks (30/treatment duration). Double immunocytochemical labeling on tissue sections from these rats used antibodies against HDAC isoforms or acetylated histones, and calbindin, a marker for PN...
November 15, 2017: Brain Research
https://www.readbyqxmd.com/read/28840369/novel-histone-deacetylase-8-selective-inhibitor-1-3-4-oxadiazole-alanine-hybrid-induces-apoptosis-in-breast-cancer-cells
#20
Vijaya Rao Pidugu, Nagendra Sastry Yarla, Anupam Bishayee, Arunasree M Kalle, Alapati Krishna Satya
Identification of isoform-specific histone deacetylase inhibitors (HDACi) is a significant advantage to overcome the adverse side effects of pan-HDACi for the treatment of various diseases, including cancer. We have designed, and synthesized novel 1,3,4 oxadiazole with glycine/alanine hybrids as HDAC8-specific inhibitors and preliminary evaluation has indicated that 1,3,4 oxadiazole with alanine hybrid [(R)-2-amino-N-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)propanamide (10b)] to be a potent HDAC8 inhibitor. In the present study, the in vitro efficacy of the molecule in inhibiting the cancer cell proliferation and the underlying molecular mechanism was studied...
August 24, 2017: Apoptosis: An International Journal on Programmed Cell Death
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