keyword
MENU ▼
Read by QxMD icon Read
search

Histone deacetylase (HDAC) inhibitors

keyword
https://www.readbyqxmd.com/read/29142427/cinnamaldehyde-cinnamic-acid-and-cinnamyl-alcohol-the-bioactives-of-cinnamomum-cassia-exhibit-hdac8-inhibitory-activity-an-in-vitro-and-in-silico-study
#1
Mangesh Patil, Amit S Choudhari, Savita Pandita, Md Ataul Islam, Prerna Raina, Ruchika Kaul-Ghanekar
Background: The altered expression of histone deacetylase family member 8 (HDAC8) has been found to be linked with various cancers, thereby making its selective inhibition a potential strategy in cancer therapy. Recently, plant secondary metabolites, particularly phenolic compounds, have been shown to possess HDAC inhibitory activity. Objective: In the present work, we have evaluated the potential of cinnamaldehyde (CAL), cinnamic acid (CA), and cinnamyl alcohol (CALC) (bioactives of Cinnamomum) as well as aqueous cinnamon extract (ACE), to inhibit HDAC8 activity in vitro and in silico...
October 2017: Pharmacognosy Magazine
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
#2
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
#3
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/29138868/hdac-inhibitor-lmk%C3%A2-235-promotes-the-odontoblast-differentiation-of-dental-pulp-cells
#4
Zhao Liu, Ting Chen, Qianqian Han, Ming Chen, Jie You, Fuchun Fang, Ling Peng, Buling Wu
The role of dental pulp cells (DPCs) in hard dental tissue regeneration had received increasing attention because DPCs can differentiate into odontoblasts and other tissue‑specific cells. In recent years, epigenetic modifications had been identified to serve an important role in cell differentiation, and histone deacetylase (HDAC) inhibitors have been widely studied by many researchers. However, the effects of HDAC4 and HDAC5 on the differentiation of DPCs and the precise molecular mechanisms remain unclear...
November 14, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29137331/hdac-inhibitors-enhance-the-immunotherapy-response-of-melanoma-cells
#5
Laurence Booth, Jane L Roberts, Andrew Poklepovic, John Kirkwood, Paul Dent
We focused on the ability of the pan-histone deacetylase (HDAC) inhibitors AR42 and sodium valproate to alter the immunogenicity of melanoma cells. Treatment of melanoma cells with HDAC inhibitors rapidly reduced the expression of multiple HDAC proteins as well as the levels of PD-L1, PD-L2 and ODC, and increased expression of MHCA. In a cell-specific fashion, melanoma isolates released the immunogenic protein HMGB1 into the extracellular environment. Very similar data were obtained in ovarian and H&NSCC PDX isolates, and in established tumor cell lines from the lung and kidney...
October 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29136455/lbh589-inhibits-glioblastoma-growth-and-angiogenesis-through-suppression-of-hif-1%C3%AE-expression
#6
Zhi-Gang Yao, Wen-Huan Li, Fang Hua, Hong-Xia Cheng, Miao-Qing Zhao, Xi-Chao Sun, Ye-Jun Qin, Jia-Mei Li
Glioblastoma (GBM) is an angiogenic malignancy with a highly unfavorable prognosis. Angiogenesis in GBM represents an adaptation to a hypoxic microenvironment and is correlated with tumor growth, invasion, clinical recurrence, and lethality. LBH589 (also called panobinostat) is a histone deacetylase (HDAC) inhibitor with potent antitumor activity. In the current study, we investigated the mechanism and effects of LBH589 on GBM growth and hypoxia-induced angiogenesis in vitro and in vivo. To determine the antitumor and angiogenesis activity and mechanism of LBH589, we used cell proliferations in vitro and GBM xenografts in vivo...
December 1, 2017: Journal of Neuropathology and Experimental Neurology
https://www.readbyqxmd.com/read/29135940/comparative-proteomic-analysis-of-lysine-acetylation-in-fish-cik-cells-infected-with-aquareovirus
#7
Hong Guo, Jie Zhang, Yaping Wang, Chen Bu, Yanyan Zhou, Qin Fang
Grass carp (Ctenopharyngodon idellus) is an important worldwide commercial freshwater culture species. However, grass carp reovirus (GCRV) causes serious hemorrhagic disease in fingerlings and yearlings of fishes. To understand the molecular pathogenesis of host cells during GCRV infection, intensive proteomic quantification analysis of lysine acetylation in Ctenopharyngodon idella kidney (CIK) cells was performed. Using dimethylation labeling-based quantitative proteomics, 832 acetylated proteins with 1391 lysine acetylation sites were identified in response to GCRV infection, among which 792 proteins with 1323 sites were quantifiable...
November 14, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29135083/comparison-of-the-anticancer-properties-of-a-novel-valproic-acid-prodrug-to-leading-histone-deacetylase-inhibitors
#8
Nataly Tarasenko, Hanna Chekroun-Setti, Abraham Nudelman, Ada Rephaeli
The HDAC inhibitory activity of valproic acid (VPA) has led to on-going evaluation of it as an anticancer agent. The histone deacetylase (HDAC) inhibitor AN446, a prodrug of VPA, releases the acid upon metabolic degradation. AN446 is >60 fold more potent than VPA in killing cancer cells in vitro. Herein, we compare the activities of AN446, as an anticancer agent, to those of representative types from each of the four major classes of HDAC inhibitors (HDACIs): vorinostat, romidepsin, entinostat and VPA. AN446 exhibited the greatest selectivity and HDAC inhibitory activity against cancer cells...
November 14, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29133060/recent-advances-in-the-discovery-of-potent-and-selective-hdac6-inhibitors
#9
REVIEW
Xiu-Xiu Wang, Ren-Zhong Wan, Zhao-Peng Liu
Histone deacetylase HDAC6, a member of the class IIb HDAC family, is unique among HDAC enzymes in having two active catalytic domains, and has unique physiological function. In addition to the modification of histone, HDAC6 targets specific substrates including α-tubulin and HSP90, and are involved in protein trafficking and degradation, cell shape and migration. Selective HDAC6 inhibitors are an emerging class of pharmaceuticals due to the involvement of HDAC6 in different pathways related to neurodegenerative diseases, cancer, and immunology...
October 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29124315/the-class-i-iv-hdac-inhibitor-mocetinostat-increases-tumor-antigen-presentation-decreases-immune-suppressive-cell-types-and-augments-checkpoint-inhibitor-therapy
#10
David Briere, Niranjan Sudhakar, David M Woods, Jill Hallin, Lars D Engstrom, Ruth Aranda, Harrah Chiang, Andressa L Sodré, Peter Olson, Jeffrey S Weber, James G Christensen
Checkpoint inhibitor therapy has led to major treatment advances for several cancers including non-small cell lung cancer (NSCLC). Despite this, a significant percentage of patients do not respond or develop resistance. Potential mechanisms of resistance include lack of expression of programmed death ligand 1 (PD-L1), decreased capacity to present tumor antigens, and the presence of an immunosuppressive tumor microenvironment. Mocetinostat is a spectrum-selective inhibitor of class I/IV histone deacetylases (HDACs), a family of proteins implicated in epigenetic silencing of immune regulatory genes in tumor and immune cells...
November 9, 2017: Cancer Immunology, Immunotherapy: CII
https://www.readbyqxmd.com/read/29120081/structure-activity-relationship-of-propargylamine-based-hdac-inhibitors
#11
Matthias Wünsch, Johanna Senger, Philipp Schultheisz, Sabrina Schwarzbich, Karin Schmidtkunz, Carmela Michalek, Michaela Klaß, Stefanie Goskowitz, Philipp Borchert, Lucas Praetorius, Wolfgang Sippl, Manfred Jung, Norbert Sewald
As histone deacetylases (HDACs) play an important role in cancer treatment, their selective inhibition has been subject of various studies. The continuous investigations have spawned a large collection of pan- and selective HDAC inhibitors, containing diverse FDA approved representatives. In former studies, a class of alkyne based inhibitors of HDACs was presented. We modified this scaffold in two previously neglected regions and compared cytotoxicity and affinity towards HDAC1, HDAC6 and HDAC8. We could show that (R)-configured propargylamines contribute increased selectivity on HDAC6, while the size of the substituents decreases their affinity...
November 9, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29118323/valproic-acid-sensitizes-hepatocellular-carcinoma-cells-to-proton-therapy-by-suppressing-nrf2-activation
#12
Jeong Il Yu, Changhoon Choi, Sung-Won Shin, Arang Son, Ga-Haeng Lee, Shin-Yeong Kim, Hee Chul Park
Although efficacy of combined histone deacetylase (HDAC) inhibitors and conventional photon radiotherapy is being tested in clinical trials, their combined effect with proton beam radiotherapy has yet to be determined. Here, we compared combined effect of valproic acid (VPA), a class I and II HDAC inhibitor and antiepileptic drug with proton and photon irradiation in hepatocellular carcinoma (HCC) cells in vitro and in vivo. We found that VPA sensitized more Hep3B cells to proton than to photon irradiation...
November 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29117473/largazole-analogues-as-histone-deacetylases-inhibitors-and-anticancer-agents-an-overview-on-structure-activity-relationships
#13
Giulio Poli, Romano Di Fabio, Luca Ferrante, Vincenzo Summa, Maurizio Botta
Since the time of its identification, the natural compound largazole rapidly caught the attention of the medicinal chemistry community for its impressive potency as histone deacetylases (HDACs) inhibitor and its strong antiproliferative activity against a broad panel of cancer cell lines. The design of largazole analogues is an expanding field of study, due to their remarkable potential as novel anticancer therapeutics. At present, a large ensemble of largazole analogues has been reported in literature, thus allowing the identification of important structure-activity relationships (SAR) that can guide the design of novel compounds with improved HDAC inhibitory profile, anticancer activity and pharmacokinetic properties...
November 8, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29115561/inhibition-of-histone-deacetylase-1-ameliorates-renal-tubulointerstitial-fibrosis-via-modulation-of-inflammation-and-extracellular-matrix-gene-transcription-in-mice
#14
Tùng Nguyễn-Thanh, Dal Kim, Sik Lee, Won Kim, Sung Kwang Park, Kyung Pyo Kang
Renal tubulointerstitial fibrosis is characterized by sustained inflammation and excessive extracellular matrix (ECM) accumulation, leading to chronic kidney disease. Valproic acid (VPA) has anticancer activity through regulation of cell differentiation and apoptosis via inhibition of histone deacetylase (HDAC) activity and is considered a class I HDAC inhibitor. In this study, the effect of VPA on unilateral ureteral obstruction (UUO)‑induced renal fibrosis by modulation of renal inflammation and ECM gene transcription was investigated...
October 27, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29115461/histone-deacetylase-inhibition-of-cardiac-autophagy-in-rats-on-a-high%C3%A2-fat-diet-with-low%C3%A2-dose-streptozotocin-induced-type-2-diabetes-mellitus
#15
Ting-I Lee, Kuan-Jen Bai, Yao-Chang Chen, Ting-Wei Lee, Cheng-Chih Chung, Wen-Chih Tsai, Shin-Yi Tsao, Yu-Hsun Kao
Autophagy serves a role in preserving cellular homeostasis. Diabetes mellitus (DM) impairs cardiac autophagy and is associated with an accumulation of cytotoxic proteins that may provoke apoptosis and damage cardiomyocytes. Histone deacetylase (HDAC) inhibitors attenuate cardiac fibrosis and inflammation, and improve cardiomyopathy resulting from DM. However, the effect of HDAC inhibition on autophagy in DM cardiomyopathy has not been investigated. The purpose of the present study was to evaluate whether HDAC inhibition modulates cardiac autophagy and to investigate the potential mechanisms in type 2 DM (T2DM) hearts...
October 26, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29114207/histone-deacetylase-inhibitors-are-protective-in-acute-but-not-in-chronic-models-of-ototoxicity
#16
Chao-Hui Yang, Zhiqi Liu, Deanna Dong, Jochen Schacht, Dev Arya, Su-Hua Sha
Previous studies have reported that modification of histones alters aminoglycoside-induced hair cell death and hearing loss. In this study, we investigated three FDA-approved histone deacetylase (HDAC) inhibitors (vorinostat/SAHA, belinostat, and panobinostat) as protectants against aminoglycoside-induced ototoxicity in murine cochlear explants and in vivo in both guinea pigs and CBA/J mice. Individually, all three HDAC inhibitors reduced gentamicin (GM)-induced hair cell loss in a dose-dependent fashion in explants...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29113288/hdac6-inhibitor-wt161-downregulates-growth-factor-receptors-in-breast-cancer
#17
Teru Hideshima, Ralph Mazitschek, Jun Qi, Naoya Mimura, Jen-Chieh Tseng, Andrew L Kung, James E Bradner, Kenneth C Anderson
We have shown that WT-161, a histone deacetylase 6 (HDAC6) inhibitor, shows remarkable anti-tumor activity in multiple myeloma (MM) in preclinical models. However, its activity in other type of cancers has not yet been shown. In this study, we further evaluated the biologic sequelae of WT161 in breast cancer cell lines. WT161 triggers apoptotic cell death in MCF7, T47D, BT474, and MDA-MB231 cells, associated with decreased expression of EGFR, HER2, and ERα and downstream signaling. However, HDAC6 knockdown shows that cytotoxicity and destabilization of these receptors triggered by WT161 are not dependent on HDAC6 inhibition...
October 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/29113227/low-dose-valproic-acid-with-low-dose-gemcitabine-augments-mhc-class-i-related-chain-a-b-expression-without-inducing-the-release-of-soluble-mhc-class-i-related-chain-a-b
#18
Tomoharu Miyashita, Kenji Miki, Takashi Kamigaki, Isamu Makino, Hidehiro Tajima, Shinichi Nakanuma, Hironori Hayashi, Hiroyuki Takamura, Sachio Fushida, Ali K Ahmed, John W Harmon, Tetsuo Ohta
To improve natural killer group 2 member D (NKG2D)-dependent cytotoxicity, the inhibition of cleavage and release of major histocompatibility complex class 1-related chain (MIC) molecules from the tumor surface are required. Valproic acid (VPA), a histone deacetylase (HDAC) inhibitor, is able to induce cell-surface MICA/B on tumor cells. In the present study, the ability of VPA and gemcitabine (GEM) to upregulate MICA/B in pancreatic cancer cells was investigated, resulting in the inhibition of cleavage and release of MIC molecules from the tumor surface...
November 2017: Oncology Letters
https://www.readbyqxmd.com/read/29113202/ezh2-and-histone-deacetylase-inhibitors-induce-apoptosis-in-triple-negative-breast-cancer-cells-by-differentially-increasing-h3-lys-27-acetylation-in-the-bim-gene-promoter-and-enhancers
#19
Julia P Huang, Kun Ling
Enhancer of zeste homolog 2 (EZH2), a subunit of polycomb repressive complex 2, is a histone methyl-transferase and is considered to work cooperatively with histone deacetylases (HDACs) in the same protein complex to mediate gene transcription repression by increasing histone H3 Lys(27) trimethylation (H3K27me3), in particular in the nucleosome (s). EZH2 is overexpressed in numerous types of cancer, including triple negative breast cancer (TNBC), a subtype of breast cancer, which there are no effective treatment options for...
November 2017: Oncology Letters
https://www.readbyqxmd.com/read/29111742/increased-post-translational-lysine-acetylation-of-myelin-basic-protein-is-associated-with-peak-neurological-disability-in-a-mouse-experimental-autoimmune-encephalomyelitis-model-of-multiple-sclerosis
#20
Ryan Lillico, Ting Zhou, Tina Khorshid Ahmad, Nicholas Stesco, Kiana Gozda, Jessica Truong, Jiming Kong, Ted M Lakowski, Michael Namaka
Citrullination of arginine residues is a post-translational modification (PTM) found on myelin basic protein (MBP), which neutralizes MBPs positive charge, and is implicated in myelin damage and multiple sclerosis (MS). Here we identify lysine acetylation as another neutralizing PTM to MBP that may be involved in myelin damage. We quantify changes in lysine and arginine PTMs on MBP derived from mice induced with an experimental autoimmune encephalomyelitis (EAE) model of MS using liquid chromatography tandem mass spectrometry...
November 7, 2017: Journal of Proteome Research
keyword
keyword
70361
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"