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Hdac 5

Wei-Sheng Chen, Wen-Jin Xu, Hua-Qiang Zhu, Lei Gao, Miao-Jun Lai, Fu-Qiang Zhang, Wen-Hua Zhou, Hui-Fen Liu
Histone acetylation and other modifications of the chromatin are important regulators of gene expression and may contribute to drug-induced behaviors and neuroplasticity. Inhibition of histone deacetylases (HDAC) activity results in the change of some drug-induced behaviors,however, relatively little is known about the effects of HDAC inhibitors on heroin-seeking behavior. In the present study, male rats were trained to self-administer heroin under a FR1 schedule for consecutive 14 days, followed by 14 daily 2hours extinction session in the operant chamber...
October 11, 2016: Brain Research
Simona Panella, Maria Elena Marcocci, Ignacio Celestino, Sergio Valente, Clemens Zwergel, Domenica Donatella Li Puma, Lucia Nencioni, Antonello Mai, Anna Teresa Palamara, Giovanna Simonetti
AIM: Histone deacetylases (HDACs) regulate the life-cycle of several viruses. We investigated the ability of different HDAC-inhibitors, to interfere with influenza virus A/Puerto Rico/8/34/H1N1 (PR8 virus) replication in Madin-Darby canine kidney and NCI cells. RESULTS: 3-(5-(3-Fluorophenyl)-3-oxoprop-1-en-1-yl)-1-methyl-1H-pyrrol-2-yl)-N-hydroxyacrylamide (MC1568) inhibited HDAC6/8 activity and PR8 virus replication, with decreased expression of viral proteins and their mRNAs...
October 14, 2016: Future Medicinal Chemistry
Rob De Vreese, Lisa Galle, Yves Depetter, Jorick Franceus, Tom Desmet, Kristof Van Hecke, Veronick Benoy, Ludo Van Den Bosch, Matthias D'hooghe
Histone deacetylase 6 (HDAC6) selective inhibitors represent an emerging class of pharmaceuticals due to the involvement of HDAC6 in different pathways related to neurodegenerative diseases, cancer and immunology. In this paper, the synthesis of a series of ten new benzohydroxamic acids, constructed employing the benzothiazepine core as a privileged pharmacophoric unit, is described. This is the first report on the synthesis and isolation of octahydrodibenzothiazepines and octahydro-6H-benzocyclo¬heptathiazepines as novel heterocyclic scaffolds, which were consecutively used to develop a new class of HDAC6 inhibitors...
October 7, 2016: Chemistry: a European Journal
P Larsson, I Alwis, B Niego, M Sashindranath, P Fogelstrand, M C L Wu, L Glise, M Magnusson, M Daglas, N Bergh, S P Jackson, R L Medcalf, S Jern
BACKGROUND: The endogenous fibrinolytic system has rarely been considered as a target to prevent thrombotic disease. Tissue plasminogen activator (t-PA) is potently increased by histone deacetylase (HDAC) inhibitors in endothelial cells in vitro, but whether this translates into increased vascular t-PA production and an enhanced fibrinolytic capacity in vivo is unknown. OBJECTIVES: The aim of this study was to determine if the HDAC inhibitor valproic acid (VPA) stimulates production of t-PA in the vasculature of mice, and further, if VPA pre-treatment affects fibrin deposition and clot formation after mechanical vessel injury...
October 5, 2016: Journal of Thrombosis and Haemostasis: JTH
Hana Čipčić Paljetak, Linda Tomašković, Mario Matijašić, Mirjana Bukvić, Andrea Fajdetić, Donatella Verbanac, Mihaela Perića
5-LOX - 5-lipoxygenase; ACT - artemisinin-based combination therapies; ADME - absorption, distribution, metabolism and excretion; BAL - broncho alveolar lavage; CABP - community acquired bacterial pneumonia; cAMP - cyclic adenosine monophosphate; CAP - community-acquired pneumonia; CF - cystic fibrosis, BOS bronchiolitis obliterans syndrome; cGMP - cyclic guanosine monophosphate; COPD - chronic obstructive pulmonary disease; COX - cyclooxygenase; DPB - diffuse panbronchiolitis; HDACs - histone deacetylases; IBD - inflammatory bowel disease; IL-1p - interleukin 1p; IL-6 - interleukin 6; MIC - minimal inhibitory concentrations; MLSB - macrolide, lincosamide, streptogramin B; NSAIDs - non-steroidal anti-inflammatory drugs; OVA - ovalbumin; PDE4 - phosphodiesterase 4; PMA - phorbol 12-myristate 13-acetate; RA - rheumatoid arthritis; RTI - respiratory tract infections; SAHA - suberoylanilide hydroxamic acid; SAR - structure-activity-relationship; Th1 - type 1 helper T-cell; TNBS - trinitrobenzene sulfonic acid; TNF-α - tumour necrosis factor α; UN - United Nations, WHO - World Health Organisation...
September 27, 2016: Current Topics in Medicinal Chemistry
Jessica A Engel, Amy J Jones, Vicky M Avery, Subathdrage D M Sumanadasa, Susanna S Ng, David P Fairlie, Tina Skinner-Adams, Katherine T Andrews
No abstract text is available yet for this article.
May 30, 2016: International Journal for Parasitology, Drugs and Drug Resistance
Silvio Holzner, Daniel Senfter, Serena Stadler, Anna Staribacher, Chi Huu Nguyen, Anna Gaggl, Silvana Geleff, Nicole Huttary, Sigurd Krieger, Walter Jäger, Helmut Dolznig, Robert M Mader, Georg Krupitza
Since cancer cells, when grown as spheroids, display drug sensitivity and radiation resistance patterns such as seen in vivo we recently established a three‑dimensional (3D) in vitro model recapitulating colorectal cancer (CRC)-triggered lymphatic endothelial cell (LEC)‑barrier breaching to study mechanisms of intra‑/extravasation. CRC metastasizes not only through lymphatics but also through blood vessels and here we extend the 3D model to the interaction of blood endothelial cells (BECs) with naïve and 5‑fluorouracil (5‑FU)‑resistant CRC CCL227 cells...
September 20, 2016: Oncology Reports
Vijaya Rao Pidugu, Nagendra Sastry Yarla, Srinivasa Rao Pedada, Arunasree M Kalle, A Krishna Satya
Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring. Of the four oxadiazoles known, 1,3,4-oxadiazole has become an important structural motif for the development of new drugs and the compounds containing 1,3,4-oxadiazole cores have a broad spectrum of biological activity. Herein, we describe the design, synthesis and biological evaluation of a series of novel 2,5-disubstituted 1,3,4-oxadiazoles (10a-10j) as class I histone deacetylase (HDAC) inhibitors...
November 1, 2016: Bioorganic & Medicinal Chemistry
Jing Shen, Shengru Wu, Wei Guo, Saisai Liang, Xueyuan Li, Xiaojun Yang
Inflammatory response which can be mediated by inflammatory genes, can be induced by pathogenic microorganisms, be associated with enteric diseases and the loss of growth performance in broilers. The understanding of epigenetic regulation of inflammatory genes could help explain the response to infection of microorganisms and inhibit the reaction of inflammation in broilers. This study investigated the effect of histone acetylation by histone deacetylases (HDAC) inhibitors trichostain A (TSA) and DNA methylation by demethylation agent 5-Aza-2'-deoxycytidine (AZA) and methyl donor methionine (Met) and folic acid (FA) on the expression of pro-inflammatory cytokines in lipopolysaccharide (LPS)-stimulated peripheral blood mononuclear cells (PBMC) from healthy broilers...
September 18, 2016: Immunobiology
Natascia Guida, Giusy Laudati, Luigi Mascolo, Ornella Cuomo, Serenella Anzilotti, Rossana Sirabella, Marianna Santopaolo, Mario Galgani, Paolo Montuori, Gianfranco Di Renzo, Lorella M T Canzoniero, Luigi Formisano
Ethylmercury thiosalicylate (thimerosal) is an organic mercury-based compound commonly used as an antimicrobial preservative that has been found to be neurotoxic. In contrast, histone deacetylases (HDACs) inhibition has been found to be neuroprotective against several environmental contaminants, such as polychlorinated biphenyls, di-2-ethylhexyl phthalate, and methylmercury. The aim of this study was to investigate the effect of HDAC inhibition on thimerosal-induced neurotoxicity in neuroblastoma cells and cortical neurons...
September 22, 2016: Toxicological Sciences: An Official Journal of the Society of Toxicology
Walter Hanel, Robert Briski, Charles W Ross, Thomas F Anderson, Mark S Kaminski, Alexandra C Hristov, Ryan A Wilcox
BACKGROUND: Cutaneous T-cell lymphomas (CTCL), with few exceptions, remain incurable and treatment is largely palliative. We performed a retrospective analysis of systemic treatment outcomes of patients diagnosed with MF/SS at the University of Michigan. METHODS: We identified 223 patients with MF/SS evaluated at the University of Michigan from 1997-2013. Disease stage at diagnosis, time of treatment, treatments received and reasons for treatment cessation were retrospectively analyzed using our CTCL database...
September 20, 2016: American Journal of Hematology
Xingsheng Hu, Lin Wang, Lin Lin, Xiaohong Han, Guifang Dou, Zhiyun Meng, Yuankai Shi
OBJECTIVE: This phase I study was to evaluate safety, maximum tolerated dose, pharmacokinetics and preliminary antitumor activity of chidamide, a novel subtype-selective histone deacetylase (HDAC) inhibitor, in combination with paclitaxel and carboplatin in patients with advanced non-small cell lung cancer (NSCLC). METHODS: Ten patients received oral chidamide 20, 25, or 30 mg twice per week continuously with paclitaxel (175 mg/m(2)) and carboplatin [area under the curve (AUC) 5 mg/mL/min] administered in a 3-week cycle...
August 2016: Chinese Journal of Cancer Research, Chung-kuo Yen Cheng Yen Chiu
Andrew J Yee, William I Bensinger, Jeffrey G Supko, Peter M Voorhees, Jesus G Berdeja, Paul G Richardson, Edward N Libby, Ellen E Wallace, Nicole E Birrer, Jill N Burke, David L Tamang, Min Yang, Simon S Jones, Catherine A Wheeler, Robert J Markelewicz, Noopur S Raje
BACKGROUND: Histone deacetylase (HDAC) inhibitors are an important new class of therapeutics for treating multiple myeloma. Ricolinostat (ACY-1215) is the first oral selective HDAC6 inhibitor with reduced class I HDAC activity to be studied clinically. Motivated by findings from preclinical studies showing potent synergistic activity with ricolinostat and lenalidomide, our goal was to assess the safety and preliminary activity of the combination of ricolinostat with lenalidomide and dexamethasone in relapsed or refractory multiple myeloma...
September 16, 2016: Lancet Oncology
Dan Gong, Wei Li, Liang-Ding Hu, Jian-Liang Shen, Mei-Yun Fang, Qing-Ming Yang, Heng-Xiang Wang, Xiao-Yan Ke, Hui-Ren Chen, Zhao Wang, Hui Liu, Feng Liu, Yi-Gai Ma, Jing-Wen Wang, Hong-Hua Li, Quan-Shun Wang, Yu Jing, Xiao-Ning Gao, Li-Ping Dou, Yong-Hui Li, Jian-Min Luo, Li Yu
BACKGROUND: The survival of patients with acute myeloid leukemia (AML) with t(8;21) was reported to be shorter in China than in other countries. PATIENTS: We analyzed the correlation between different cytarabine (Ara-c) regimens and outcome in 255 t(8;21) AML patients in China who received postremission consolidation chemotherapy only. RESULTS: The 5-year overall survival (OS) of the high-dose Ara-c group (HDAC; 2≤ Ara-c ≤3 g/m2), intermediate-dose Ara-c group (MDAC; 1...
September 17, 2016: Acta Haematologica
Qin Xu, Dakshesh Patel, Xian Zhang, Richard D Veenstra
Histone deacetylase (HDAC) inhibitors are small molecule anti-cancer therapeutics that exhibit limiting cardiotoxicities including QT interval prolongation and life-threatening cardiac arrhythmias. Because the molecular mechanisms for HDAC inhibitor-induced cardiotoxicity are poorly understood, we performed whole cell patch voltage clamp experiments to measure cardiac sodium currents (INa) from wild-type neonatal mouse ventricular or human induced pluripotent stem cell derived cardiomyocytes treated with trichostatin A (TSA), vorinostat (VOR), or romidepsin (FK228)...
September 16, 2016: American Journal of Physiology. Heart and Circulatory Physiology
Julian C Bahr, Robert W Robey, Victoria Luchenko, Agnes Basseville, Arup R Chakraborty, Hanna Kozlowski, Gary T Pauly, Paresma Patel, Joel P Schneider, Michael M Gottesman, Susan E Bates
We previously demonstrated activation of the mitogen-activated protein kinase (MAPK) pathway in a series of romidepsin-selected T-cell lymphoma cell lines as a mechanism of resistance to the histone deacetylase inhibitor (HDI), romidepsin. As Ras mutation leads to activation of both the MAPK and the phosphoinositide 3-kinase (PI3K) pathway, we examined whether combining romidepsin with small molecule pathway inhibitors would lead to increased apoptosis in cancers harboring Ras mutations. We treated 18 Ras mutant or wild-type cell lines with romidepsin in the presence of a MEK inhibitor (PD-0325901) and/or an AKT inhibitor (MK-2206) and examined apoptosis by flow cytometry...
September 13, 2016: Oncotarget
Leslie A Garrett, Whitfield B Growdon, Bo R Rueda, Rosemary Foster
BACKGROUND: Pre-clinical studies have demonstrated that natural and synthetic histone deacetylase (HDAC) inhibitors can impede the in vitro and in vivo growth of cell lines from a variety of gynecologic and other malignancies. We investigated the anti-tumor activity of panobinostat (LBH589) both in vitro and in vivo as either a single agent or in combination with conventional cytotoxic chemotherapy using patient-derived xenograft (PDX) models of primary serous ovarian tumors. METHODS: The ovarian cancer cell lines OVCAR8, SKOV3 and their paclitaxel-resistant derivatives OVCAR8-TR and SKOV3-TR were treated with increasing doses of LBH589...
2016: Journal of Ovarian Research
Obdulia Rabal, Juan A Sánchez-Arias, Mar Cuadrado-Tejedor, Irene de Miguel, Marta Pérez-González, Carolina García-Barroso, Ana Ugarte, Ander Estella-Hermoso de Mendoza, Elena Sáez, Maria Espelosin, Susana Ursua, Tan Haizhong, Wu Wei, Xu Musheng, Ana Garcia-Osta, Julen Oyarzabal
Simultaneous inhibition of phosphodiesterase 5 (PDE5) and histone deacetylases (HDAC) has recently been validated as a potentially novel therapeutic approach for Alzheimer's disease (AD). To further extend this concept, we designed and synthesized the first chemical series of dual acting PDE5 and HDAC inhibitors, and we validated this systems therapeutics approach. Following the implementation of structure- and knowledge-based approaches, initial hits were designed and were shown to validate our hypothesis of dual in vitro inhibition...
October 13, 2016: Journal of Medicinal Chemistry
Haeseong Park, Ignacio Garrido-Laguna, Aung Naing, Siqing Fu, Gerald S Falchook, Sarina A Piha-Paul, Jennifer J Wheler, David S Hong, Apostolia M Tsimberidou, Vivek Subbiah, Ralph G Zinner, Ahmed O Kaseb, Shreyaskumar Patel, Michelle A Fanale, Vivianne M Velez-Bravo, Funda Meric-Bernstam, Razelle Kurzrock, Filip Janku
Preclinical models suggest that histone deacetylase (HDAC) and mammalian target of rapamycin (mTOR) inhibitors have synergistic anticancer activity. We designed a phase I study to determine the safety, maximum tolerated dose (MTD), recommended phase II dose (RP2D), and dose-limiting toxicities (DLTs) of combined mTOR inhibitor sirolimus (1 mg-5 mg PO daily) and HDAC inhibitor vorinostat (100 mg-400 mg PO daily) in patients with advanced cancer. Seventy patients were enrolled and 46 (66%) were evaluable for DLT assessment since they completed cycle 1 without dose modification unless they had DLT...
August 31, 2016: Oncotarget
Yudibeth Sixto-López, Martiniano Bello, Rolando Alberto Rodríguez-Fonseca, Martha Cecilia Rosales-Hernández, Marlet Martínez-Archundia, José Antonio Gómez-Vidal, José Correa-Basurto
HDAC are a family of proteins involved in the deacetylation of histones and other non-histones substrates. HDAC6 belong to class II and share similar biological functions with others of its class. Nevertheless, its three dimensional structure that involves the catalytic site remains unknown for explore the ligand recognition properties. Therefore, in this contribution, homology modeling, 100 ns-long Molecular Dynamics (MD) simulation and docking calculations were combined to explore the conformational complexity and binding properties of the catalytic domain 2 from HDAC6 (DD2-HDAC6), for which activity and affinity towards 5 different ligands has been reported...
September 2, 2016: Journal of Biomolecular Structure & Dynamics
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