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Histone Deacetylase InhibitorsHistone DeacetylasesHistonesHistone Deacetylase 1Hydroxamic AcidsHistone Deacetylase 2AcetylationHistone AcetyltransferasesChromatinSin3 Histone Deacetylase and Corepressor ComplexValproic AcidRepressor ProteinsButyratesDepsipeptidesEnzyme InhibitorsNucleosomesHistone CodeMethylationEpigenesis, GeneticHistone DemethylasesHistone-Lysine N-MethyltransferaseTranscription, GeneticHistone ChaperonesSirtuinsMi-2 Nucleosome Remodeling and Deacetylase ComplexGene SilencingCell Line, TumorSirtuin 1Chromatin Assembly and DisassemblyTranscription FactorsChromatin ImmunoprecipitationAcetyltransferasesp300-CBP Transcription FactorsProtein BindingSirtuin 2Nuclear ProteinsDNA-Binding ProteinsGene Expression RegulationPhenylbutyratesDNA MethylationMolecular Sequence DataHeLa CellsSaccharomyces cerevisiae ProteinsCell LineProtein Processing, Post-TranslationalJumonji Domain-Containing Histone DemethylasesRetinoblastoma-Binding Protein 4HeterochromatinProtein MethyltransferasesChromosomal Proteins, Non-HistonePromoter Regions, GeneticApoptosisButyric AcidAmino Acid SequenceCell CycleAzacitidineNuclear Receptor Co-Repressor 1Transcriptional ActivationAntineoplastic AgentsProtein Structure, TertiarySaccharomyces cerevisiaeBlotting, WesternRNA, MessengerMutationIsobutyratesCell ProliferationCyclin-Dependent Kinase Inhibitor p21Cell Cycle ProteinsBenzamidesBase SequenceRNA, Small InterferingPhosphorylationGene Expression Regulation, NeoplasticReverse Transcriptase Polymerase Chain ReactionCells, CulturedDown-RegulationDrug SynergismGene Expression Regulation, FungalDNACREB-Binding ProteinBinding SitesCell DifferentiationRNA InterferenceImmunoprecipitationDNA (Cytosine-5-)-MethyltransferaseTumor Cells, CulturedTrans-ActivatorsRetinoblastoma-Binding Protein 7TransfectionEuchromatinSignal TransductionGenes, ReporterSp1 Transcription FactorModels, BiologicalEpigenomicsMethyltransferasesE1A-Associated p300 ProteinMEF2 Transcription FactorsGene Expression Regulation, EnzymologicNuclear Receptor Co-Repressor 2
HDACsAcetylationChromatinInhibitorsLysineInhibitorAcetyl groupsProteinsDeacetylationHDAC4EnzymesTailsClassMethylFoundModificationsRoleHDACDeacetylation of histonesEpigeneticInhibit histone deacetylaseLysine residuesTranscriptionGenesPost-translationalHda1ChromosomesExpressionCorrelatesGene regulationAmino-terminalPathwaysDrugsActivityOppositeTargetImportantDevelopmentGroupsAbilityIncreaseBrain
HDACs11
Acetylation15
Chromatin3
Inhibitors6
  • Histone Deacetylase Inhibitors" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • This graph shows the total number of publications written about "Histone Deacetylase Inhibitors" by people in Harvard Catalyst Profiles by year, and whether "Histone Deacetylase Inhibitors" was a major or minor topic of these publication. (harvard.edu)
  • Below are the most recent publications written about "Histone Deacetylase Inhibitors" by people in Profiles. (harvard.edu)
  • The impact of histone deacetylase inhibitors on immune cells and implications for cancer therapy. (harvard.edu)
  • Histone deacetylase inhibitors enhance oncolytic herpes simplex virus therapy for malignant meningioma. (harvard.edu)
  • How do histone deacetylase inhibitors work? (turningtooneanother.net)
Lysine4
  • Histone deacetylases (EC 3.5.1.98, HDAC) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on both histone and non-histone proteins. (wikipedia.org)
  • HDAC proteins are now also called lysine deacetylases (KDAC), to describe their function rather than their target, which also includes non-histone proteins. (wikipedia.org)
  • Histone tails are normally positively charged due to amine groups present on their lysine and arginine amino acids. (wikipedia.org)
  • Post-translational modification of histones, in particular the removal or addition of acetyl groups on ϵ-N-acetyl lysine residues, play an important role in epigenetic regulation of transcription. (biomedcentral.com)
Inhibitor8
  • Nitrilase mediated mild hydrolysis of a carbon-14 nitrile for the radiosynthesis of 4-(7-hydroxycarbamoyl-[1-14 C-heptanoyl]-oxy)-benzoic acid methyl ester, [14 C]-SHP-141: A novel class I/II histone deacetylase (HDAC) inhibitor. (harvard.edu)
  • The drug, known as a histone deacetylase (HDAC) inhibitor, blocks the removal of acetyl groups, and researchers Wang et al. (bipolarnews.org)
  • Valproate, in addition to its properties as a mood-stabilizing anticonvulsant that increases brain GABA levels and exerts a variety of other neurobiological effects, is also a histone deacetylase inhibitor. (bipolarnews.org)
  • TMP195 is an inhibitor of class IIa histone deacetylase (HDAC) with IC50 of 15 nM - 59 nM for HDAC4, 5, 7 and 9. (csnpharm.cn)
  • Tinostamustine is an alkylatlng histone-deacetylase inhibitor (HDACi) fusion molecule. (csnpharm.cn)
  • It is a functional pan-histone-deacetylase inhibitor and is assumed to potentiate the alkylating activity of the compound and/or may help to overcome resistance to other therapeutic agents. (csnpharm.cn)
  • Theophylline is a natural product present in tea and cocoa, working as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. (csnpharm.cn)
  • Nanatinostat is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC). (csnpharm.cn)
Acetyl groups1
  • Histone deacetylases remove those acetyl groups, increasing the positive charge of histone tails and encouraging high-affinity binding between the histones and DNA backbone. (wikipedia.org)
Proteins3
  • Together with the acetylpolyamine amidohydrolases and the acetoin utilization proteins, the histone deacetylases form an ancient protein superfamily known as the histone deacetylase superfamily. (wikipedia.org)
  • Histones (biology) are highly alkaline proteins that are found in cells nuclei that package and order the Deoxyribonucleic acid into nucleosomes. (histoready.com)
  • DNA is tightly wrapped around histones, which regulates access for subsequent translation into proteins. (biologists.com)
Deacetylation1
HDAC41
  • Histone deacetylase 4 (HDAC4) has been shown to be a key regulator of chondrocyte hypertrophy during skeletogenesis. (biomedcentral.com)
Enzymes1
  • The current experiments were designed to investigate the effects of Zyflamend on the expression of class I and II histone deacetylases, a family of enzymes known to be over expressed in a variety of cancers. (biomedcentral.com)
Tails1
  • These positive charges help the histone tails to interact with and bind to the negatively charged phosphate groups on the DNA backbone. (wikipedia.org)
Class3
Methyl1
  • Environmental events such as stress or exposure to chemicals can bring about epigenetic changes by adding or subtracting acetyl or methyl groups from strands of DNA or the histones around which it is wound. (bipolarnews.org)
Found1
Modifications1
Role1
  • Histones also playing a role in gene regulation and occur in all eukaryotes. (histoready.com)
HDAC15
  • Histone deacetylases (EC 3.5.1.98, HDAC) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on both histone and non-histone proteins. (wikipedia.org)
  • HDAC proteins are now also called lysine deacetylases (KDAC), to describe their function rather than their target, which also includes non-histone proteins. (wikipedia.org)
  • HDACs, are classified in four classes depending on sequence homology to the yeast original enzymes and domain organization: HDAC (except class III) contain zinc and are known as Zn2+-dependent histone deacetylases. (wikipedia.org)
  • Histone deacetylase (HDAC) inhibitors can induce differentiation, cell cycle and growth arrest or in certain cases apoptosis in cancer cells. (nature.com)
  • The acetylation status of histones is determined by histone deacetylase (HDAC), and HDAC are strongly expressed in cancerous tissue. (novapublishers.com)
  • The mitotic deacetylase complex (MiDAC) is a recently identified histone deacetylase (HDAC) complex. (elifesciences.org)
  • In this study, we show that statins inhibited the histone deacetylase (HDAC) activity and increased the accumulation of acetylated histone-H3 and the expression of p21 WAF/CIP in human cancer cells. (aacrjournals.org)
  • These results suggest a novel mechanism for statins through abrogation of the HDAC activity and promoter histone-H3 acetylation to regulate p21 expression. (aacrjournals.org)
  • The enzymes controlling the state of histone acetylation in vivo are histone acetyltransferase (HAT) and histone deacetylases (HDAC). (anti-agingfirewalls.com)
  • HDAC enzymes catalyze the removal of acetyl groups from the amino-terminal lysine residues of core nucleosomal histones. (anti-agingfirewalls.com)
  • One reason for the current interest in HAT and HDAC is that histone deacetylase inhibitors appear to act as powerful inducers of differentiation or apoptosis in cancer cells. (anti-agingfirewalls.com)
  • Histone acetylation and deacetylation are implicated in a number of the theories of aging treated in my ANTI-AGING FIREWALLS - THE SCIENCE AND TECHNOLOGY OF LONGEVITY treatise, We find a number of HAT and HDAC inhibitors in the anti-aging firewall dietary regimen . (anti-agingfirewalls.com)
  • HDAC inhibitors are drugs that can affect what genes are active by interacting with proteins in chromosomes called histones . (cancer.org)
  • The molecular mechanism that underlies its clinical efficacy remains controversial and is complicated by the broad range of intracellular effects of valproic acid, including its ability to inhibit histone deacetylase (HDAC) and induce protein chaperone expression. (mcmaster.ca)
  • ZOLINZA is a histone deacetylase (HDAC) inhibitor indicated for the treatment of cutaneous manifestations in patients with cutaneous T-cell lymphoma (CTCL) who have progressive, persistent or recurrent disease on or following two systemic therapies. (nih.gov)
Deacetylation of histones3
  • Lysines 9 and 14 of histone H3 and lysines 5, 8 and 16 of H4 are acetylated in active chromatin and hypoacetylated in silenced chromatin, and overexpression of Sir2 promotes global deacetylation of histones, indicating that Sir2 may be a histone deacetylase. (nih.gov)
  • Acetylation and deacetylation of histones play an important role in transcription regulation. (novapublishers.com)
  • Histone deacetylases are enzymes responsible for the deacetylation of histones, which can directly regulate transcription, and have been implicated in AD pathology. (umd.edu)
Epigenetic7
  • The most well-characterized alteration is DNA hypermethylation, and a modification of histones also contributes to tumor suppressor loss through epigenetic silencing. (novapublishers.com)
  • Histone post-translational modifications have been implicated in many biological functions and diseases and serve an important role in epigenetic regulation of gene expression. (umd.edu)
  • Aberrant modulations in histone post-translational have been suggested to occur in the brain as part of Alzheimer's disease (AD) pathology, consistent with the epigenetic blockade of neurodegeneration. (umd.edu)
  • This body of work aims to better elucidate the epigenetic pathology of AD and to aid in identification of histone-modifying enzymes involved in AD pathology for drug targets and treatment options. (umd.edu)
  • Epigenetic regulators often constitute chromatin-modifying enzymes which catalyze the addition and removal of posttranslational modifications on histones and are involved in the control of gene expression by modulating chromatin structure and function. (elifesciences.org)
  • Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. (drugbank.com)
  • Interplay between histone acetylation and deacetylation is one of the key components in epigenetic regulation of transcription. (ppjonline.org)
Inhibit histone deacetylase1
  • E )-Resveratrol appears to inhibit histone deacetylase activity in a concentration-dependent manner according to a recent research publication . (anti-agingfirewalls.com)
Lysine residues1
  • Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). (drugbank.com)
Transcription2
  • Generally, histone deacetylation in conjunction with concomitant histone methylation is associated with repression of genes, whereas high levels of histone acetylation correlates with active transcription of genes, although there are a few exception to this rule ( Bannister and Kouzarides, 2011 ). (ppjonline.org)
  • Little is known, however, about the relative roles of methylation and histone deacetylase activity in the stable inhibition of transcription on densely methylated endogenous promoters, such as those for silenced alleles of imprinted genes, genes on the female inactive X chromosome and tumour-suppressor genes inactivated in cancer cells. (johnshopkins.edu)
Genes4
  • Histone acetylation is a chemical modification of a portion of a histone which leads to selective unwrapping of the DNA making the exposed genes amenable to activation and expression. (anti-agingfirewalls.com)
  • The result is that even if NF-kappaB gets into a cell's nucleus, the wrapped-up histones keep it from activating genes that lead to inflammation and other age-related damage. (anti-agingfirewalls.com)
  • Thus, although DNA methylation and histone deacetylation appear to act as synergistic layers for the silencing of genes in cancer, dense CpG island methylation is dominant for the stable maintenance of a silent state at these loci. (johnshopkins.edu)
  • When histones undergo chemical modifications such as acetylation (the addition of an acetyl group), this changes how DNA is packed and thus how genes are read, or expressed. (nih.gov)
Post-translational1
  • For the changes in post-translational modifications observed, structural mechanisms were proposed to explain alterations in the DNA-histone affinity in the nucleosome, which can modulate gene expression. (umd.edu)
Hda12
  • Here we report the requirement of Mo-HDA1-mediated histone deacetylation during asexual development and pathogenesis for the rice blast fungus, Magnaporthe oryzae . (ppjonline.org)
  • Structural similarity and phylogenetic analysis suggested that MoHDA1 is an ortholog of Saccharomyces cerevisiae Hda1, which is a representative member of class II histone deacetylases. (ppjonline.org)
Chromosomes1
Expression4
Correlates1
  • Furthermore, we use chemical derivatives of valproic acid to show that the ability to promote GRP78 levels directly correlates with the induction of histone H4 hyperacetylation. (mcmaster.ca)
Gene regulation1
  • Histones also playing a role in gene regulation and occur in all eukaryotes. (histoready.com)
Amino-terminal1
  • Mutational studies indicate that lysine 16 in the amino-terminal tail of histone H4 and lysines 9, 14 and 18 in H3 are critically important in silencing, whereas lysines 5, 8 and 12 of H4 have more redundant functions. (nih.gov)
Pathways1
  • Histone deacetylase is involved in a series of pathways within the living system. (wikipedia.org)
Drugs1
  • Drugs that increase histone acetylation can reverse cognitive decline in animal models. (nih.gov)
Activity4
  • Our analysis of two SIR2 mutations supports the idea that this deacetylase activity accounts for silencing, recombination suppression and extension of life span in vivo. (nih.gov)
  • recent research suggesting that microRNAs and over-activity of histone deacetylases may be root causes of the auto-immune disease systemic lupus erythematosus (SLE). (anti-agingfirewalls.com)
  • It activates protein deacetylase SIRT1, and this is thought to be the main reason why it has anti-aging activity( ref ). (anti-agingfirewalls.com)
  • The methyl-CpG-binding protein MeCP2 appears to reside in a complex with histone deacetylase activity. (johnshopkins.edu)
Opposite2
Target1
  • SIRT6 interacts with the NF-kappaB RELA subunit and deacetylates histone H3 lysine 9 (H3K9) at NF-kappaB target gene promoters. (anti-agingfirewalls.com)
Important1
  • Taken together, our data suggest that MoHDA1-dependent histone deacetylation is important for efficient asexual development and infection of host plants in M. oryzae . (ppjonline.org)
Development1
  • This dissertation details the development and optimization of unique protein standards for quantification, called quantification concatamers, for the absolute quantification of histone deacetylase isoforms in human frontal cortex with AD, human neural retina with AD and age-related macular degeneration, and whole brain hemisphere of a 5XFAD mouse model of AD. (umd.edu)
Groups2
  • Histone tails are normally positively charged due to amine groups present on their lysine and arginine amino acids. (wikipedia.org)
  • These positive charges help the histone tails to interact with and bind to the negatively charged phosphate groups on the DNA backbone. (wikipedia.org)
Ability1
  • Acetylation, which occurs normally in a cell, neutralizes the positive charges on the histone by changing amines into amides and decreases the ability of the histones to bind to DNA. (wikipedia.org)
Increase1
  • Comparison of acetylation levels for H3K9 and H3K14 showed that lack of MoHDA1 gene led to significant increase in H3K9 and H3K14 acetylation level, compared to the wild-type and complementation strain, confirming that it is a bona fide histone deacetylase. (ppjonline.org)
Brain1
  • Studies in animals have linked a process called histone acetylation in brain cells to cognitive decline. (nih.gov)