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Histone deacetylase inhibitor

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https://www.readbyqxmd.com/read/28102705/the-acetyl-code-in-rheumatoid-arthritis-and-other-rheumatic-diseases
#1
Chiara Angiolilli, Dominique L Baeten, Timothy R Radstake, Kris A Reedquist
Growing evidence supports the idea that aberrancies in epigenetic processes contribute to the onset and progression of human immune-mediated inflammatory diseases, such as rheumatoid arthritis (RA). Epigenetic regulators of histone tail modifications play a role in chromatin accessibility and transcriptional responses to inflammatory stimuli. Among these, histone deacetylases (HDACs) regulate the acetylation status of histones and nonhistone proteins, essential for immune responses. Broad-spectrum HDAC inhibitors are well-known anti-inflammatory agents and reduce disease severity in animal models of arthritis; however, selective HDAC inhibitors remain poorly studied...
January 19, 2017: Epigenomics
https://www.readbyqxmd.com/read/28102109/epigenetic-regulation-of-rgs2-regulator-of-g-protein-signaling-2-in-chemoresistant-ovarian-cancer-cells
#2
Ercan Cacan
Regulator of G-protein signaling 2 (RGS2) is a GTPase-activating protein functioning as an inhibitor of G-protein coupled receptors (GPCRs). RGS2 dysregulation was implicated in solid tumour development and RGS2 downregulation has been reported in prostate and ovarian cancer progression. However, the molecular mechanism by which RGS2 expression is suppressed in ovarian cancer remains unknown. The expression and epigenetic regulation of RGS2 in chemosensitive and chemoresistant ovarian cancer cells were determined by qRT-PCR and chromatin immunoprecipitation assays, respectively...
January 19, 2017: Journal of Chemotherapy
https://www.readbyqxmd.com/read/28101176/anticancer-effects-of-valproic-acid-on-oral-squamous-cell-carcinoma-via-sumoylation-in-vivo-and-in-vitro
#3
Zhijian Sang, Yang Sun, Hong Ruan, Yong Cheng, Xiaojun Ding, Youcheng Yu
Aberrant histone deacetylase (HDAC) has a key role in the neoplastic process associated with the epigenetic patterns of tumor-related genes. The present study was performed to investigate the effects and determine the mechanism of action of the HDAC inhibitor, valproic acid (VPA), on the CAL27 cell line derived from oral squamous cell carcinoma (OSCC). The effects of VPA on the viability of CAL27 cells were investigated using MTT assays. Alterations in the cell cycle and apoptosis were also examined using propidium iodide (PI) and Annexin V-PI assays, and were subequently analyzed by flow cytometry...
December 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28100329/-protective-effect-of-histone-acetylation-against-cortical-injury-in-neonatal-rats
#4
Ji-Chong Huang, Ya-Fei Li, Feng-Yan Zhao, Yi Qu, De-Zhi Mu
OBJECTIVE: To investigate the protective effect of histone acetylation against hypoxic-ischemic cortical injury in neonatal rats. METHODS: A total of 90 neonatal rats aged 3 days were divided into three groups: sham-operation, cortical injury model, and sodium butyrate (a histone deacetylase inhibitor) treatment. The rats in the model and the sodium butyrate treatment groups were intraperitoneally injected with lipopolysaccharide (0.05 mg/kg), and then right common carotid artery ligation was performed 2 hours later and the rats were put in a hypoxic chamber (oxygen concentration 6...
January 2017: Zhongguo Dang Dai Er Ke za Zhi, Chinese Journal of Contemporary Pediatrics
https://www.readbyqxmd.com/read/28099914/advances-in-epigenetic-glioblastoma-therapy
#5
Dong Hoon Lee, Hyun-Wook Ryu, Hye-Rim Won, So Hee Kwon
Glioblastoma multiforme (GBM) is the most lethal primary brain tumor in adults despite contemporary gold-standard first-line treatment strategies. This type of tumor recurs in virtually all patients and no commonly accepted standard treatment exists for the recurrent disease. Therefore, advances in all scientific and clinical aspects of GBM are urgently needed. Epigenetic mechanisms are one of the major factors contributing to the pathogenesis of cancers, including glioblastoma. Epigenetic modulators that regulate gene expression by altering the epigenome and non-histone proteins are being exploited as therapeutic drug targets...
January 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/28099388/valproic-acid-mitigates-the-inflammatory-response-and-prevents-acute-respiratory-distress-syndrome-in-a-murine-model-of-escherichia-coli-pneumonia-at-the-expense-of-bacterial-clearance
#6
George Kasotakis, Manuel Galvan, Elizabeth King, Beda Sarkar, Arthur Stucchi, Joseph P Mizgerd, Peter A Burke, Daniel Remick
BACKGROUND: Histone deacetylase inhibitors (HDACI) are members of a family of epigenetic modifying agents with broad anti-inflammatory properties. These anti-inflammatory properties may have important therapeutic implications in Acute Respiratory Distress Syndrome (ARDS). However, administration of HDACI may create an immunosuppressive environment conducive to bacterial growth. Accordingly, the aim of the current study is to investigate the effect of HDACI Valproic Acid (VPA) on host inflammatory response and bacterial burden in a murine model of E...
January 18, 2017: Journal of Trauma and Acute Care Surgery
https://www.readbyqxmd.com/read/28099148/suberoylanilide-hydroxamic-acid-increases-anti-cancer-effect-of-tumor-necrosis-factor-%C3%AE-through-up-regulation-of-tnf-receptor-1-in-lung-cancer-cells
#7
Bo Ra You, Bo Ram Han, Woo Hyun Park
Suberoylanilide hydroxamic acid (SAHA) as a histone deacetylase (HDAC) inhibitor has anti-cancer effect. Here, we evaluated the effect of SAHA on HDAC activity and cell growth in many normal lung and cancer cells. We observed that the HDAC activities of lung cancer cells were higher than that of normal lung cells. SAHA inhibited the growth of lung cancer cells regardless of the inhibitory effect on HDAC. This agent induced a G2/M phase arrest and apoptosis, which was accompanied by mitochondrial membrane potential (MMP: ΔΨm) loss in lung cancer cells...
January 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28094843/hypomethylating-agents-in-combination-with-histone-deacetylase-inhibitors-in-higher-risk-myelodysplastic-syndromes-is-there-a-light-at-the-end-of-the-tunnel
#8
EDITORIAL
Maximilian Stahl, Amer M Zeidan
No abstract text is available yet for this article.
January 17, 2017: Cancer
https://www.readbyqxmd.com/read/28094841/phase-2-randomized-double-blind-study-of-pracinostat-in-combination-with-azacitidine-in-patients-with-untreated-higher-risk-myelodysplastic-syndromes
#9
Guillermo Garcia-Manero, Guillermo Montalban-Bravo, Jesus G Berdeja, Yasmin Abaza, Elias Jabbour, James Essell, Roger M Lyons, Farhad Ravandi, Michael Maris, Brian Heller, Amy E DeZern, Sunil Babu, David Wright, Bertrand Anz, Ralph Boccia, Rami S Komrokji, Philip Kuriakose, James Reeves, Mikkael A Sekeres, Hagop M Kantarjian, Richard Ghalie, Gail J Roboz
BACKGROUND: The prognosis of patients with higher risk myelodysplastic syndromes (MDS) remains poor despite available therapies. Histone deacetylase inhibitors have demonstrated activity in patients with MDS and in vitro synergy with azacitidine. METHODS: A phase 2 randomized, placebo-controlled clinical trial of azacitidine and pracinostat was conducted in patients who had International Prognostic Scoring System intermediate-2-risk or high-risk MDS. The primary endpoint was the complete response (CR) rate by cycle 6 of therapy...
January 17, 2017: Cancer
https://www.readbyqxmd.com/read/28092474/novel-histone-deacetylase-6-hdac6-selective-inhibitors-a-patent-evaluation-wo2014181137
#10
Claudia A Simões-Pires, Philippe Bertrand, Muriel Cuendet
The invention described in this patent (WO2014181137) is related to hydroxamic acid derivatives with inhibitory activity towards histone deacetylases (HDACs), their synthetic process and pharmaceutical formulations, as well as a method for treating patients suffering from a list of selected tumoral, inflammatory, cardiac and chronic disorders. HDACs are known to deacetylate histones and other proteins, which makes HDAC inhibitors able to affect cell survival, cell signaling, transport, and gene expression. Those effects have been associated to the therapeutic success of HDAC inhibitors...
January 16, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28089578/dual-influences-of-early-life-maternal-deprivation-on-histone-deacetylase-activity-and-recognition-memory-in-rats
#11
Manoel Osório Albuquerque Filho, Betânia Souza de Freitas, Rebeca Carvalho Lacerda Garcia, Pedro Castilhos de Freitas Crivelaro, Nadja Schröder, Maria Noêmia Martins de Lima
Exposure to stress early in life may negatively impact nervous system functioning, including increasing the proneness to learning and memory impairments later in life. Maternal deprivation, a model of early-life stress, hinders memory in adult rats and lessens brain-derived neurotrophic factor (BDNF) levels in the hippocampus in a very heterogeneous way among individuals. The main goal of the present study was to investigate the possible epigenetic modulation underlying recognition memory impairment and reduced BDNF levels in the hippocampus of adult maternally deprived rats...
January 9, 2017: Neuroscience
https://www.readbyqxmd.com/read/28086911/enhanced-neuroinflammation-mediated-by-dna-methylation-of-the-glucocorticoid-receptor-triggers-cognitive-dysfunction-after-sevoflurane-anesthesia-in-adult-rats-subjected-to-maternal-separation-during-the-neonatal-period
#12
Yangzi Zhu, Yu Wang, Rui Yao, Ting Hao, Junli Cao, He Huang, Liwei Wang, Yuqing Wu
BACKGROUND: Mounting evidence indicates that children who experience abuse and neglect are prone to chronic diseases and premature mortality later in life. One mechanistic hypothesis for this phenomenon is that early life adversity alters the expression or functioning of the glucocorticoid receptor (GR) throughout the course of life and thereby increases sensitivity to inflammatory stimulation. An exaggerated pro-inflammatory response is generally considered to be a key cause of postoperative cognitive dysfunction (POCD)...
January 7, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28079009/emerging-roles-of-calreticulin-in-cancer-implications-for-therapy
#13
Kavya Venkateswaran, Amit Verma, Anant Narayan Bhatt, Anju Shrivastava, Kailash Manda, Hanumantharao G Raj, Ashok Prasad, Christophe Len, Virinder S Parmar, Bilikere Dwarakanath
Calreticulin (CRT), initially identified as a ubiquitous calcium-binding protein in the endoplasmic reticulum, has emerged as a multifunctional protein with roles in calcium homeostasis, molecular chaperoning and cell adhesion. Emerging evidence suggests its involvement in tumorigenesis facilitating proliferation, migration, and adhesion. CRT translocated to the cell surface (ecto-CRT) serves as a phagocytic signal for immunogenic cell death (ICD) mediated through dendritic cells (DCs) and cytotoxic T-cell activation thereby making tumors susceptible to immunotherapy-based anti-cancer strategies...
January 11, 2017: Current Protein & Peptide Science
https://www.readbyqxmd.com/read/28078999/hdacs-and-hdac-inhibitors-in-urothelial-carcinoma-perspectives-for-an-antineoplastic-treatment
#14
Maria Pinkerneil, Michèle J Hoffmann, Wolfgang A Schulz, Günter Niegisch
Histone deacetylases (HDACs) influence diverse cellular processes and may contribute to tumor development and progression by multiple mechanisms. Class I HDACs are often overexpressed in cancers contributing to a genome-wide epigenetic state permitting increased proliferation, and diminished apoptosis and cell differentiation. Class IIA and IIB isoenzymes may likewise contribute to tumorigenesis as components of specific intranuclear repressor complexes or regulators of posttranslational protein modifications...
January 11, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28078985/designing-isoform-selective-inhibitors-against-classical-hdacs-for-effective-anticancer-therapy-insight-and-perspectives-from-in-silico
#15
Shabir Ahmad Ganai
Histone deacetylase inhibitors, the small molecules modulating the biological activity of histone deacetylases are emerging as potent chemotherapeutic agents. Despite their considerable therapeutic benefits in disease models, the lack of isoform specificity culminates in debilitating off target effects, raising serious concerns regarding their applicability. This emphasizes the pressing and unmet medical need of designing isoform selective inhibitors for safe and effective anticancer therapy. Keeping these grim facts in view, the current article sheds light on structural basis of off-targeting...
12, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28077797/repression-of-fyn-related-kinase-in-breast-cancer-cells-is-associated-with-promoter-site-specific-cpg-methylation
#16
Edward T Bagu, Sayem Miah, Chenlu Dai, Travis Spriggs, Yetunde Ogunbolude, Erika Beaton, Michelle Sanders, Raghuveera K Goel, Keith Bonham, Kiven E Lukong
The triple-negative breast cancer subtype is highly aggressive and has no defined therapeutic target. Fyn-related kinase (FRK) is a non-receptor tyrosine kinase, reported to be downregulated in breast cancer and gliomas, where it is suggested to have tumor suppressor activity. We examined the expression profile of FRK in a panel of 40 breast cancer cells representing all the major subtypes, as well as in 4 non-malignant mammary epithelial cell lines. We found that FRK expression was significantly repressed in a proportion of basal B breast cancer cell lines...
January 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28073598/hdac10-as-a-potential-therapeutic-target-in-ovarian-cancer
#17
Muhtadi M Islam, Tapahsama Banerjee, Colin Z Packard, Shweta Kotian, Karuppaiyah Selvendiran, David E Cohn, Jeffrey D Parvin
OBJECTIVE: We analyzed histone deacetylase 10 (HDAC10) for function in the context of the DNA damage response in BRCA1-null ovarian cancer cells as well as evaluated the potential of general HDAC inhibitors in primary ovarian carcinoma cells. HDAC10 had previously been shown to be highly stimulatory to the process of homology directed repair in HeLa cells, and in this study we investigated whether HDAC10 could impact in vitro the response to anticancer therapies. We hypothesized that the loss of HDAC10 would sensitize cells to platinum therapy...
January 7, 2017: Gynecologic Oncology
https://www.readbyqxmd.com/read/28071906/single-conformation-spectroscopy-of-suberoylanilide-hydroxamic-acid-saha-a-molecule-bites-its-tail
#18
Di Zhang, Karl N Blodgett, Xiao Zhu, Timothy S Zwier
Suberoylanilide hydroxamic acid (C6H5NHCO(CH2)6CONHOH, SAHA) is a histone deacetylase inhibitor that causes growth arrest and differentiation of many tumor types and is an approved drug for the treatment of cancer. With a hydrogen-bonding amide group adjacent to its phenyl ring "head", and a hydroxamic acid group at the "tail" end of a C6 alkyl chain linker, SAHA possesses an interesting potential energy landscape to be probed by single-conformation methods. The alkyl chain's preference for extended structures is in competition with tail-to-head (T-H) or head-to-tail (H-T) hydrogen bonds between the amide and hydroxamic acid groups...
January 10, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28070968/bacterial-short-chain-fatty-acid-metabolites-modulate-the-inflammatory-response-against-infectious-bacteria
#19
R O Corrêa, A Vieira, E M Sernaglia, M Lancellotti, A T Vieira, M J Avila-Campos, H G Rodrigues, M A R Vinolo
Short chain fatty acids (SCFAs), predominately acetic, propionic and butyric acids, are bacterial metabolites with an important role in the maintenance of homeostasis due to their metabolic and immunomodulatory actions. Some evidence suggests that they may also be relevant during infections. Therefore, we aimed to investigate the effects of SCFAs in the effector functions of neutrophils to an opportunistic pathogenic bacteria, Aggregatibacter actinomycetemcomitans (A. actinomycetemcomitans). Using a subcutaneous model to generate a mono, isolated infection of A...
January 9, 2017: Cellular Microbiology
https://www.readbyqxmd.com/read/28067178/histone-deacetylase-inhibitors-for-the-treatment-of-colorectal-cancer-recent-progress-and-future-prospects
#20
Avineesh Singh, Preeti Patel, Vijay K Patel, Deepak K Jain, Ravichandran Veerasamy, Prabodh C Sharma, Harish Rajak
Colorectal cancer is a devastating disease with a dismal prognosis which is heavily hampered by delayed diagnosis. Surgical resection, radiation therapy and chemotherapy are the curative options. Due to few therapeutic treatments available i.e., mono and combination therapy and development of resistance towards drug response, novel and efficacious therapy is urgently needed. Histone deacetylase inhibitors (HDACIs) are emerging class of therapeutic agents having potential anticancer activity with minimal toxicity for different types of malignancies in preclinical studies...
January 9, 2017: Current Cancer Drug Targets
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