Non-Hydroxamate Histone Deacetylase Inhibitors [PDF]
Current Medicinal Chemistry, 2005 A number of histone deacetylase (HDAC) inhibitors have been developed as anticancer agents and most of them are hydroxamic acid derivatives, typified by suberoylanilide hydroxamic acid (SAHA), Trichostatin A (TSA) and NVP-LAQ824. However, hydroxamic acids have been associated with poor pharmacokinetics and severe toxicity. In addition, although isozyme-
Takayoshi, Suzuki, Naoki, Miyata
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In vitro Enzymatic Assays of Histone Decrotonylation on Recombinant Histones
Bio-Protocol, 2018 Class I histone deacetylases (HDACs) are efficient histone decrotonylases, broadening the enzymatic spectrum of these important (epi-)genome regulators and drug targets. Here, we describe an in vitro approach to assaying class I HDACs with different acyl-
Rachel Fellows, Patrick Varga-Weisz
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Protein acetylation in archaea, bacteria, and eukaryotes [PDF]
, 2010 Proteins can be acetylated at the alpha-amino group of the N-terminal amino acid (methionine or the penultimate amino acid after methionine removal) or at the epsilon-amino group of internal lysines.
Lainio, Jarmo +1 more
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Phase I dose-escalation study of the mTOR inhibitor sirolimus and the HDAC inhibitor vorinostat in patients with advanced malignancy. [PDF]
, 2016 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 ...
Falchook, Gerald S. +17 more
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Chemical phylogenetics of histone deacetylases [PDF]
Nature Chemical Biology, 2010 The broad study of histone deacetylases in chemistry, biology and medicine relies on tool compounds to derive mechanistic insights. A phylogenetic analysis of class I and II histone deacetylases (HDACs) as targets of a comprehensive, structurally diverse panel of inhibitors revealed unexpected isoform selectivity even among compounds widely perceived ...
Bradner, James E. +6 more
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Emerging roles of telomeric chromatin alterations in cancer [PDF]
, 2019 Telomeres, the nucleoprotein structures that cap the ends of eukaryotic chromosomes, play important and multiple roles in tumorigenesis. Functional telomeres need the establishment of a protective chromatin structure based on the interplay between the ...
Biroccio, Annamaria +2 more
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Histone deacetylase inhibitors suppress mutant p53 transcription via histone deacetylase 8 [PDF]
Oncogene, 2012 Mutation of the p53 gene is the most common genetic alteration in human cancer and contributes to malignant process by enhancing transformed properties of cells and resistance to anticancer therapy. Mutant p53 is often highly expressed in tumor cells at least, in part, due to its increased half-life.
Yan, Wensheng +6 more
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Nature Communications, 2016 SIRT7 is a member of sirtuin family proteins that are described as NAD+-dependent class III histone deacetylases. Here, the authors show that SIRT7 is histone desuccinylase catalysing H3K122 desuccinylation, thereby promoting chromatin condensation and ...
Lei Li +14 more
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An RNA-seq transcriptome analysis of histone modifiers and RNA silencing genes in soybean during floral initiation process. [PDF]
PLoS ONE, 2013 Epigenetics has been recognised to play vital roles in many plant developmental processes, including floral initiation through the epigenetic regulation of gene expression.
Lim Chee Liew +2 more
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Activation of AMP-activated protein kinase by metformin induces protein acetylation in prostate and ovarian cancer cells [PDF]
, 2016 AMP-activated protein kinase (AMPK) is an energy sensor and master regulator of metabolism. AMPK functions as a fuel gauge monitoring systemic and cellular energy status.
Galdieri, Luciano +3 more
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