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317 results for “Histone deacetylase”
Human Histone Deacetylase 6 (HDAC6); A Target Enabling Package
<p>HDAC6 is a cytosolic deacetylase with diverse roles in cellular trafficking, autophagy and cell signalling. Specifically targeting the unique zinc-finger ubiquitin-binding domain (ZnF-UBD) of HDAC6 may be an attractive strategy in myeloma and lymphoma but no inhibitor has been reported to date. Presented here are 4 co-crystal structures of HDAC6 ZnF-UBD in complex with different compounds, and associated SPR, ITC and FP assays.</p>
Selective Estrogen Receptor Modulators to Enhance the Efficacy of Viral Reactivation With Histone Deacetylase Inhibitors
ClinicalTrials.gov study NCT03382834. IPD Sharing: YES. Countries: 2. Publications: 1.
Data from: Diverse nucleosome site-selectivity among histone deacetylase complexes
<p>Histone acetylation regulates chromatin structure and gene expression and is removed by histone deacetylases (HDACs). HDACs are commonly found in various protein complexes to confer distinct cellular functions, but how the multi-subunit complexes influence deacetylase activities and site-selectivities in chromatin is poorly understood. Recent studies on the HDAC1 containing CoREST complex and acetylated nucleosome substrates revealed a notable preference for deacetylation of histone H3 acetyl-Lys9 vs. acetyl-Lys14 (M. Wu et al, 2018). Here we analyze the enzymatic properties of five class I HDAC complexes: CoREST, NuRD, Sin3B, MiDAC and SMRT with site-specific acetylated nucleosome substrates. Our results demonstrate that these HDAC complexes show a wide variety of deacetylase rates in a site-selective manner. A Gly13 in the histone H3 tail is responsible for a sharp reduction in deacetylase activity of the CoREST complex for H3K14ac. These studies provide a framework for connecting enzymatic and biological functions of specific HDAC complexes.</p>
Effect of the histone deacetylase inhibitor Trichostatin A on facial development in cichlid fishes
<p>A central question in biology is the molecular origins of phenotypic diversity. While genetic changes are key to the genotype-phenotype relationship, alterations to chromatin structure and the physical packaging of histone proteins may also be important drivers of vertebrate divergence. We investigate the impact of such an epigenetic mechanism, histone acetylation, within a textbook example of an adaptive radiation. Cichlids of Lake Malawi have adapted diverse craniofacial structures, and here we investigate how histone acetylation influences morphological variation in these fishes. Specifically, we assessed the effect of inhibiting histone deacetylation using the drug trichostatin A (TSA) on developing facial structures. We examined this during three critical developmental windows in two cichlid species with alternate adult morphologies. Exposure to TSA during neural crest cell (NCC) migration and as post-migratory NCCs proliferate into the pharyngeal arches resulted in significant changes in lateral and ventral shape in <em>Maylandia</em>, but not in <em>Tropheops</em>. This included an overall shortening of the head, widening of the lower jaw, and steeper craniofacial profile, all of which are paedomorphic morphologies. In contrast, treatment with TSA during early chondrogenesis did not result in significant morphological changes in either species. Together, these data suggest a sensitivity to epigenetic alterations that are both time- and species-dependent. We find that morphologies are due to non-autonomous or potentially indirect effects on NCC development, including in part a global developmental delay. Our research bolsters the understanding that proper histone acetylation is essential for early craniofacial development and identifies a species-specific robustness to developmental change. Overall, this study demonstrates how epigenetic regulation may play an important role in both generating and buffering morphological variation.</p>
Dietary Histone Deacetylase Inhibitors (HDAC)
ClinicalTrials.gov study NCT01543074. IPD Sharing: Not stated. Countries: 1. Publications: 1.
Exploratory Evaluation of AR-42 Histone Deacetylase Inhibitor in the Treatment of Vestibular Schwannoma and Meningioma
ClinicalTrials.gov study NCT02282917. IPD Sharing: NO. Countries: 1. Publications: 2.
Effect of the histone deacetylase inhibitor Trichostatin A on facial development in cichlid fishes
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Supplementary materials from: Histone deacetylase 2 and 3 of Sarcoptes scabiei: Characterization of a potential drug target
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Data from: Diverse nucleosome site-selectivity among histone deacetylase complexes
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Fig. 6 in Sesquiterpenes with diverse skeletons from histone deacetylase inhibitor modified cultures of the basidiomycete Cyathus stercoreus (Schwein.) De Toni HFG134
Fig. 6. (A) The four possible stereoisomers of 9. (B), (C) The comparisons of the experimental CD and calculated ECD of 9.
Study of Vorinostat (MK0683), an Histone Deacetylase (HDAC) Inhibitor in Combination With Bortezomib in Patients With Relapsed or Refractory Multiple Myeloma (MK-0683-095)
ClinicalTrials.gov study NCT00773838. IPD Sharing: YES. Countries: 0. Publications: 1.
A Dose Escalation Study of the Histone Deacetylase Inhibitor (HDACi) JNJ 26481585 in Combination With VELCADE (Bortezomib) and Dexamethasone for Patients With Relapsed Multiple Myeloma
ClinicalTrials.gov study NCT01464112. IPD Sharing: Not stated. Countries: 1. Publications: 1.
Study to Evaluate the Safety and Effect of HIVconsv Vaccines in Combination With Histone Deacetylase Inhibitor Romidepsin on the Viral Rebound Kinetic After Treatment Interruption in Early Treated HIV
ClinicalTrials.gov study NCT02616874. IPD Sharing: Not stated. Countries: 1. Publications: 1.
An Investigational Study of a Histone Deacetylase (HDAC) Inhibitor Plus Targretin in Cutaneous T-Cell Lymphoma Patients (0683-016)(TERMINATED)
ClinicalTrials.gov study NCT00127101. IPD Sharing: Not stated. Countries: 0. Publications: 1.
Data from: Lysine-14 acetylation of histone H3 in chromatin confers resistance to the deacetylase and demethylase activities of an epigenetic silencing complex
The core CoREST complex (LHC) contains histone deacetylase HDAC1 and histone demethylase LSD1 held together by the scaffold protein CoREST. Here we analyze the purified LHC with modified peptide and reconstituted semisynthetic mononucleosome substrates. LHC demethylase activity toward methyl-Lys4 in histone H3 is strongly inhibited by H3 Lys14 acetylation, and this appears to be an intrinsic property of the LSD1 subunit. Moreover, the deacetylase selectivity of LHC unexpectedly shows a marked preference for H3 acetyl-Lys9 versus acetyl-Lys14 in nucleosome substrates but this selectivity is lost with isolated acetyl-Lys H3 protein. This diminished activity of LHC for Lys14 deacetylation in nucleosomes is not merely due to steric accessibility based on the pattern of sensitivity of the LHC enzymatic complex to hydroxamic acid-mediated inhibition. Overall, these studies have revealed how a single Lys modification can confer a composite of resistance in chromatin to a key epigenetic enzyme complex involved in gene silencing.
Fig. 3 in Sesquiterpenes with diverse skeletons from histone deacetylase inhibitor modified cultures of the basidiomycete Cyathus stercoreus (Schwein.) De Toni HFG134
Fig. 3. ECD and NMR of 1 and 2.
Fig. 2. Key 2D in Sesquiterpenes with diverse skeletons from histone deacetylase inhibitor modified cultures of the basidiomycete Cyathus stercoreus (Schwein.) De Toni HFG134
Fig. 2. Key 2D NMR correlations of compounds 1–9.
Fig. 1 in Sesquiterpenes with diverse skeletons from histone deacetylase inhibitor modified cultures of the basidiomycete Cyathus stercoreus (Schwein.) De Toni HFG134
Fig. 1. The chemical structures of compounds 1–13.
Trial of the Histone-Deacetylase Inhibitor ITF2357 Followed by Mechlorethamine in Relapsed/Refractory Hodgkin's Lymphoma
ClinicalTrials.gov study NCT00792467. IPD Sharing: Not stated. Countries: 1. Publications: 0.
Histone Deacetylase Inhibitor LBH589 in Addition to Corticosteroids in Patients With Acute Graft Versus Host Disease (GVHD)
ClinicalTrials.gov study NCT01111526. IPD Sharing: Not stated. Countries: 1. Publications: 0.
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International Brain Laboratory public data
The International Brain Laboratory public data releases expose standardized mouse decision-making experiments, including Neuropixels recordings, widefield calcium imaging, behavior, and session metadata accessed through the ONE API.
OpenNeuro
OpenNeuro is a free, open platform for sharing neuroimaging datasets, with public search, dataset pages, and download paths for web, S3, DataLad, and the OpenNeuro CLI.