deacetylase inhibitors
"Shock and kill" effects of class I selective histone deacetylase inhibitors in combination with the glutathione synthesis inhibitor buthionine sulfoximine in cell line models for HIV 1 quiescence
... Histone deacetylase inhibitors (HDACIs) induce HIV-1 activation from quiescence, yet class/isoform-selective HDACIs are needed to specifically target HIV-1 ...
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HDACiDB: a database for histone deacetylase inhibitors
... histone deacetylase (HDAC) inhibitor database (HDACiDB) was constructed to enable rapid access to data relevant to the development of epigenetic modulators (HDAC inhibitors [HDACi]), helping bring precision ...
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Clinical use and applications of histone deacetylase inhibitors in multiple myeloma
... Abstract: The incorporation of various novel therapies has resulted in a significant survival benefit in newly diagnosed and relapsed patients with multiple myeloma (MM) over the past decade. Despite these advances, ...
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Quiescence Promotes Latent HIV Infection and Resistance to Reactivation from Latency with Histone Deacetylase Inhibitors
... histone deacetylase inhibitors (HDACi), such as vorinostat (20, 21) and romidepsin (22–24), which are believed to achieve reactivation through chromatin ...
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The effects of DNA methylation and histone deacetylase inhibitors on human papillomavirus early gene expression in cervical cancer, an in vitro and clinical study
... histone deacetylase inhibitors acetylate non-histone transcription regulatory proteins [26], we wanted to analyze whether these epigenetic drugs would induce changes at p53, which is a key player in HPV ...
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Acetylation site specificities of lysine deacetylase inhibitors in human cells
... Figure 2 | Specificity of KDACIs and subcellular distribution of KDACI-upregulated acetylated proteins. a, Site-based specificity analysis of KDACIs in HeLa cells. SILAC ratios of KDACI upregulated sites were used to ...
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Histone deacetylase inhibitors modulate metalloproteinase gene expression in chondrocytes and block cartilage resorption
... to penetrate the highly negatively charged cartilage matrix will also raise the effective IC 50 in the cartilage explant assay. The time points of medium collection, days 7 and 14, are those at which release of, ...
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Histone deacetylase inhibitors induce apoptosis in human eosinophils and neutrophils
... Reagents were obtained as follows: apicidin, MC-1293 and MS-275 (Alexis, Lausen, Switzerland), CD95 mono- clonal antibody (clone CH-11; Immunotech, Marseille, France), NF-kB p65 and acetyl-NF-kB p65 (Lys310) anti- bodies ...
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Histone deacetylase enzymes and selective histone deacetylase inhibitors for antitumor effects and enhancement of antitumor immunity in glioblastoma
... HDAC inhibitors when used as monotherapy have yet to yield the progression free survival results that the preclinical mechanistic evidence would suggest, with an exception to vorinostat (and even then, only ...
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Histone Deacetylase Inhibitors for Treating a Spectrum of Diseases Not Related to Cancer
... histone deacetylase in- hibitors (HDACi’s), which are being studied in models of a broad range of diseases not related to the proapoptotic properties used to treat ...
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Virtual screening and experimental validation of novel histone deacetylase inhibitors
... histone deacetylase (HDAC) activities [3, ...HDAC inhibitors have emerged as a new class of therapeutic agents and have generated much interest among pharmacologists, and cancer and diabetes re- searchers ...
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Histone deacetylase inhibitors: clinical implications for hematological malignancies
... This class of HDACis presents a different structure from the other classes because of the 2′-aminoanilide moiety, which can likely function as a weak zinc-chelating group into the tube-like active site of the ...
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Synergy between histone deacetylase inhibitors and DNA- damaging agents is mediated by histone deacetylase 2 in colorectal cancer
... Deletion of HDAC2 without drug treatment is not sufficient to induce cell death [26]. Here we show that, although HDAC2 depletion is not sufficient for cell death it leads to perturbations in the higher order chromatin ...
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Activity of histone deacetylase inhibitors and an Aurora kinase inhibitor in BCR-ABL-expressing leukemia cells: Combination of HDAC and Aurora inhibitors in BCR-ABL-expressing cells
... of HDAC proteins (Figure 2A). As such, our data indicated that vorinostat or pracinostat and tozasertib affected the activities of both Aurora kinase and HDAC, in turn in- creasing antitumor activity in this system. ...
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Interpreting clinical assays for histone deacetylase inhibitors
... A number of clinical trials have been completed and many others are ongoing using HDACi as single agents and in combination with radiotherapy and/or chemotherapy for the treatment of various hematological and solid ...
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Histone Deacetylase Inhibitors As Potential Therapeutic Agents For Various Disorders
... CBHA (Carboxycinnamic-m acid Bis-hydroxamide- HDAC inhibitor) which is also known as M-carboxycinnamic acid bishydroxamide is a potent HDAC inhibitor. It shows the structural basis for different derivatives such as ...
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Synthesis of prenyl transferase inhibitors and histone deacetylase inhibitors
... e deacetylase active site has features o f both métallo proteases and serine proteases, consistent with the contacts that TSA makes in the active site, (shown in figure ...
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Histone Deacetylase Inhibitors: Current Status in Treatment of Leukemia
... 35. Garcia-Manero G, Yang H, Bueso-Ramos C, Ferrajoli A, Cortes J, Wierda WG, Faderl S, Koller C, Morris G, Rosner G, Loboda A, Fantin VR, Randolph SS, Hardwick JS, Reilly JF, Chen C, Ricker JL, Secrist JP, Richon VM, ...
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Targeting Inflammation in Heart Failure with Histone Deacetylase Inhibitors
... HDAC inhibitors also have been shown to reduce cell death and prevent mal- adaptive ventricular remodeling in ro- dent models of MI (38–41), and in the set- ting of chronic hypertension in rats ...
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Histone deacetylase inhibitors (HDACIs): multitargeted anticancer agents
... different inhibitors has been developed that broadly inhibits several ...targeted inhibitors, we will foster anticancer modalities that are safer and more effective over the current nontargeted agents and ...
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