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https://www.readbyqxmd.com/read/28918353/antitumor-platinum-iv-derivatives-of-carboplatin-and-the-histone-deacetylase-inhibitor-4-phenylbutyric-acid
#1
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
#2
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
#3
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
#4
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-1-trial
#5
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 preclinical models, including MYC-driven ones. In this report the safety and preliminary activity results of CUDC-907, with and without rituximab, in patients with relapsed/refractory diffuse large B-cell lymphoma are presented, with a particular focus on those with MYC-altered disease. Thirty-seven diffuse large B-cell lymphoma patients were enrolled, 14 with confirmed MYC-altered disease...
August 31, 2017: Haematologica
https://www.readbyqxmd.com/read/28855102/alterations-in-histone-acetylases-and-acetylated-histone-expression-in-aging-ethanol-fed-rats
#6
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 40 weeks (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...
August 27, 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
#7
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
https://www.readbyqxmd.com/read/28838999/animacroxam-a-novel-dual-mode-compound-targeting-histone-deacetylases-and-cytoskeletal-integrity-of-testicular-germ-cell-cancer-cells
#8
Gustav Steinemann, Alexandra Dittmer, Weronika Kuzyniak, Björn Hoffmann, Mark Schrader, Rainer Schobert, Bernhard Biersack, Bianca Nitzsche, Michael Hoepfner
Novel approaches for the medical treatment of advanced solid tumors including testicular germ cell tumors (TGCT) are desperately needed. Especially, TGCT patients not responding to cisplatin-based therapy need therapeutic alternatives, as there is no effective medical treatment available for this particular subgroup. Here, we studied the suitability of the novel dual mode compound animacroxam for TGCT treatment. Animacroxam consists of a HDAC-inhibitory hydroxamate moiety coupled to a 4,5-diarylimidazole with inherent cytoskeleton disrupting potency...
August 24, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28833658/valproic-acid-functionalized-cyclometalated-iridium-iii-complexes-as-mitochondria-targeting-anticancer-agents
#9
Rui-Rong Ye, Jian-Jun Cao, Cai-Ping Tan, Liang-Nian Ji, Zong-Wan Mao
Valproic acid (VPA) is a short-chain fatty acid type histone deacetylase inhibitor (HDACi), which can cause growth arrest and induce differentiation of transformed cells. Phosphorescent cyclometalated Ir(III) complexes have emerged as potential anticancer agents. Conjugation of VPA to Ir(III) complexes by ester bond, we designed and synthesized three VPA-functionalized cyclometalated iridium(III) complexes (1a-3a). These complexes display excellent two-photon properties, which is favorable for live cell imaging...
August 22, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28829799/novel-histone-deacetylase-inhibitor-ar-42-exhibits-antitumor-activity-in-pancreatic-cancer-cells-by-affecting-multiple-biochemical-pathways
#10
Yi-Jin Chen, Wen-Hung Wang, Wan-Yu Wu, Chia-Chi Hsu, Ling-Rung Wei, Sheng-Fan Wang, Ya-Wen Hsu, Chih-Chuang Liaw, Wan-Chi Tsai
OBJECTIVE: Pancreatic cancer is one of the most lethal types of cancer with a 5-year survival rate of ~5%. Histone deacetylases (HDACs) participate in many cellular processes, including carcinogenesis, and pharmacological inhibition of HDACs has emerged as a potential therapeutic strategy. In this study, we explored antitumor activity of the novel HDAC inhibitor AR-42 in pancreatic cancer. METHODS: Human pancreatic cancer cell lines BxPC-3 and PANC-1 were used in this study...
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/28812327/design-and-synthesis-of-terephthalic-acid-based-histone-deacetylase-inhibitors-with-dual-stage-anti-plasmodium-activity
#12
Katharina Stenzel, Ming Jang Chua, Sandra Duffy, Yevgeniya Antonova-Koch, Stephan Meister, Alexandra Hamacher, Matthias U Kassack, Elizabeth Winzeler, Vicky M Avery, Thomas Kurz, Katherine T Andrews, Finn K Hansen
In this work we aimed to develop parasite-selective histone deacetylase inhibitors (HDAC) inhibitors with activity against the disease-causing asexual blood stages of Plasmodium as well as causal prophylactic and/or transmission blocking properties. We report the design, synthesis, and biological testing of a series of 13 terephthalic acid-based HDAC inhibitors. All compounds showed low cytotoxicity against human embryonic kidney (HEK293) cells (IC50 : 8->51 μm), with 11 also having sub-micromolar in vitro activity against drug-sensitive (3D7) and multidrug-resistant (Dd2) asexual blood-stage P...
August 15, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28812060/reolysin-and-histone-deacetylase-inhibition-in-the-treatment-of-head-and-neck-squamous-cell-carcinoma
#13
Alena C Jaime-Ramirez, Jun-Ge Yu, Enrico Caserta, Ji Young Yoo, Jianying Zhang, Tae Jin Lee, Craig Hofmeister, John H Lee, Bhavna Kumar, Quintin Pan, Pawan Kumar, Robert Baiocchi, Theodoros Teknos, Flavia Pichiorri, Balveen Kaur, Matthew Old
Oncolytic viruses (OVs) are emerging as powerful anti-cancer agents and are currently being tested for their safety and efficacy in patients. Reovirus (Reolysin), a naturally occurring non-pathogenic, double-stranded RNA virus, has natural oncolytic activity and is being tested in phase I-III clinical trials in a variety of tumor types. With its recent US Food and Drug Administration (FDA) orphan drug designation for several tumor types, Reolysin is a potential therapeutic agent for various cancers, including head and neck squamous cell carcinomas (HNSCCs), which have a 5-year survival of ∼55%...
June 16, 2017: Molecular Therapy Oncolytics
https://www.readbyqxmd.com/read/28791964/effect-of-copper-on-the-up-regulation-down-regulation-of-genes-cytotoxicity-and-ion-dissolution-for-mesoporous-bioactive-glasses
#14
Gurbinder Kaur, N Sriranganathan, S G Waldrop, Purnima Sharma, B N Chudasama
In the present study, copper-based (25 - x)CaO - xCuO -10P2O5 - 5B2O3 - 60SiO2 (x = 2.5, 5, 7.5, 10 mol%) mesoporous bioactive glasses (MBGs) were synthesized using the sol-gel technique with cetyltrimethyl ammonium bromide as the structure-directing agent. The live-dead cell count and cytocompatibility of MBGs for J774A.1 murine macrophages have also been investigated for different concentrations of MBGs. The ionic dissolution profile for Ca, P and Si has been evaluated in the simulated body fluid. The effect of copper content as well as the ionic dissolution products on the up-regulation and down-regulation of TGIF-2, HDAC-4, Smurf-1, mir-30c and mir-130a genes for the murine model are investigated using reverse transcription-polymerase chain reaction...
August 9, 2017: Biomedical Materials
https://www.readbyqxmd.com/read/28776290/synthesis-characterization-and-evaluation-of-cd-l-proline-2-a-novel-histone-deacetylase-inhibitor-that-induces-epigenetic-modification-of-histone-deacetylase-isoforms-in-a549-cells
#15
Anusha Chidambaram, Arunachalam Sekar, Kavya S H, Ramesh Kumar Chidambaram, Kalaiarasi Arunachalam, Senthilkumar G P, Ravikumar Vilwanathan
Histone deacetylases (HDACs) play an important role in the epigenetic regulation of gene expression through their effects on the compact chromatin structure. In clinical studies, several classes of histone deacetylase inhibitors (HDACi) have demonstrated potent anticancer activities with metal complexes. Hence, we synthesized cadmium-proline complexes using both the D- and L-isomers of proline and evaluated their biological activities by observing the efficiency of their inhibition of HDAC activity, ability to reduce the expression of HDAC isoforms in A549 cells and effect on apoptosis...
August 3, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28757400/epigenetic-regulation-of-ec-sod-expression-in-aging-lung-fibroblasts-role-of-histone-acetylation
#16
Jesse Roman, Jianxin Zhu, Jeffrey D Ritzenthaler, Igor N Zelko
Lung disorders characterized by fibroproliferation and excessive deposition of extracellular matrices occur in late adulthood, and their pathological manifestations become more prominent with aging. The exact mechanisms linking aging and fibroproliferative disorders are unknown, but increased oxidative stress resulting in the accumulation of damaged proteins, DNA, and lipids is considered a major factor. In the lung, and especially in the pulmonary fibroblasts, the extracellular superoxide dismutase (EC-SOD) is a major antioxidant enzyme that has been implicated in pulmonary fibrosing disorders, among others...
July 27, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28757101/discovery-of-a-tetrahydroisoquinoline-based-hdac-inhibitor-with-improved-plasma-stability
#17
Nan Zhou, Yugang Yan, Chunxi Liu, Jinning Hou, Wenfang Xu, Yingjie Zhang
Histone deacetylase inhibitors with desirable pharmacokinetic profiles which can be delivered to solid tumor tissues in large amount might be promising to treat solid tumor effectively. Herein, structural modification of a previously reported tetrahydroisoquinoline-based HDAC inhibitor 1 was carried out to improve its plasma stability for more feasible drug delivery. Among three newly synthesized analogs, the in vitro rat plasma stability of compound 2 (t1/2=630min) was over 5-fold improved than its parent 1 (t1/2=103min)...
June 26, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28749244/radiation-protection-and-mitigation-potential-of-phenylbutyrate-delivered-via-oral-administration
#18
Alexandra C Miller, Rafael Rivas, Robert McMahon, Karvelisse Miller, Leonard Tesoro, Vilmar Villa, Daminik Yanushkevich, Paul Lison
PURPOSE: Phenylbutyrate (PB), a histone deacetylase inhibitor (HDACi) has demonstrated radiation protection in both in vitro and in vivo models. Studies previously demonstrated that PB and other HDAC inhibitors could inhibit radiation lethality in vivo by subcutaneous (s.c) injection. The objective of this study was to test the ability of oral PB treatment to protect against or to mitigate acute gamma radiation-induced lethality in vivo. MATERIALS AND METHODS: Human osteoblasts cells were used to evaluate radiation survival when PB was delivered pre- or post-radiation...
July 27, 2017: International Journal of Radiation Biology
https://www.readbyqxmd.com/read/28743391/valporic-acid-enhances-the-atrial-natriuretic-peptide-anp-mediated-anti-hypertrophic-activity-by-modulating-the-npr1-gene-transcription-in-h9c2-cells-in-vitro
#19
Senthamizharasi Manivasagam, Tamilselvi Velusamy, Boopathi Sowndharajan, Navvi Chandrasekar, Suresh Dhanusu, Elangovan Vellaichamy
The present study was aimed to determine whether stimulating Npr1 gene activity using Valporic acid (VA), a small short chain fatty acid molecule can enhance ANP mediated anti-hypertrophic activity in isoproterenol (ISO) - treated H9c2 cells in vitro. H9c2 cells were treated with ISO (10(-5) M) and co-treated with VA (10(-5) M) in the presence and absence of ANP (10(-8)M), for 48h. ATRA (10(-5) M) was used as a positive inducer of Npr1 gene transcription. The mRNA expression of Npr1 and PKG-I genes, proto-oncogenes (c-fos, c-jun and c-myc) and hypertrophic markers (ANP, BNP, α-sk and β-MyHC), genes were determined by quantitative PCR (qPCR)...
July 22, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28720877/role-of-the-histone-deacetylase-inhibitor-valproic-acid-in-high-fat-diet-induced-hypertension-via-inhibition-of-hdac1-angiotensin-ii-axis
#20
J Choi, S Park, T K Kwon, S I Sohn, K M Park, J I Kim
BACKGROUND: Obesity is known as an epidemic worldwide because of consumption of westernized high-fat diets and one of the major risk factors of hypertension. Histone deacetylases (HDACs) control gene expression by regulating histone/non-histone protein deacetylation. HDAC inhibitors exert anti-cancer and anti-inflammatory effects and play a protective role in cardiovascular diseases. In the present study, we tested the effect of an FDA-approved pan-HDAC inhibitor valproic acid (VPA) on high-fat diet (HFD)-induced hypertension in mice...
July 19, 2017: International Journal of Obesity: Journal of the International Association for the Study of Obesity
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