Histone Deacetylase Inhibitors from Burkholderia thailandensis [PDF]
Bioactivity-guided fractionation of an extract of Burkholderia thailandensis led to the isolation and identification of a new cytotoxic depsipeptide and its dimer. Both compounds potently inhibited the function of histone deacetylases 1 and 4. The monomer, spiruchostatin C (2), was tested side by side with the clinical depsipeptide FK228 (1, Istodax,
Paul, Klausmeyer +3 more
openaire +2 more sources
ATF4‐mediated stress response as a therapeutic vulnerability in chordoma
We screened 5 chordoma cell lines against 100+ inhibitors of epigenetic and metabolic pathways and kinases and identified halofuginone, a tRNA synthetase inhibitor. Mechanistically halofuginone induces an integrated stress response, with eIF2alpha phosphorylation, activation of ATF4 and its target genes CHOP, ASNS, INHBE leading to cell death ...
Lucia Cottone +11 more
wiley +1 more source
Lysine acetylome profiling uncovers novel histone deacetylase substrate proteins in Arabidopsis
Histone deacetylases have central functions in regulating stress defenses and development in plants. However, the knowledge about the deacetylase functions is largely limited to histones, although these enzymes were found in diverse subcellular ...
Markus Hartl +15 more
doaj +1 more source
HDAC4 regulates satellite cell proliferation and differentiation by targeting P21 and Sharp1 genes [PDF]
Skeletal muscle exhibits a high regenerative capacity, mainly due to the ability of satellite cells to replicate and differentiate in response to appropriate stimuli. Epigenetic control is effective at different stages of this process.
Adamo, Sergio +9 more
core +2 more sources
Targeted modulation of IGFL2‐AS1 reveals its translational potential in cervical adenocarcinoma
Cervical adenocarcinoma patients face worse outcomes than squamous cell carcinoma counterparts despite similar treatment. The identification of IGFL2‐AS1's differential expression provides a molecular basis for distinguishing these histotypes, paving the way for personalized therapies and improved survival in vulnerable populations globally.
Ricardo Cesar Cintra +6 more
wiley +1 more source
Antiproliferative and epigenetic effects of tannic acid on MCF-7 human breast cancer cells
In breast carcinoma, epigenetic modifications, particularly disruption of histone acetylation, have become a significant research focus in recent years for discovering new treatments.
Sumeyya Deniz Aybek +2 more
doaj +1 more source
Metabolism, HDACs, and HDAC Inhibitors: A Systems Biology Perspective
Histone deacetylases (HDACs) are epigenetic enzymes that play a central role in gene regulation and are sensitive to the metabolic state of the cell.
Jacob King +2 more
doaj +1 more source
Inhibition of histone deacetylase as a treatment for cardiac hypertrophy [PDF]
The present invention provides for methods of treating and preventing cardiac hypertrophy. Class II HDACs, which are known to participate in regulation of chromatin structure and gene expression, have been shown to have beneficial effects on cardiac ...
Bristow, Michael R. +3 more
core +1 more source
Non-Peptide Macrocyclic Histone Deacetylase Inhibitors [PDF]
Inhibition of histone deacetylase inhibitors (HDACi) hold great promise in cancer therapy because of their demonstrated ability to arrest proliferation of nearly all transformed cell types. Of the several structurally distinct small molecule HDACi reported, macrocyclic depsipeptides have the most complex recognition cap-group moieties and present an ...
Adegboyega K, Oyelere +6 more
openaire +2 more sources
SIRT4 positively regulates autophagy via ULK1, but independently of HDAC6 and OPA1
Cells expressing SIRT4 (H161Y), a catalytically inactive mutant of the sirtuin SIRT4, fail to upregulate LC3B‐II and exhibit a reduced autophagic flux under stress conditions. Interestingly, SIRT4(H161Y) promotes phosphorylation of ULK1 at S638 and S758 that are associated with inhibition of autophagy initiation.
Isabell Lehmkuhl +13 more
wiley +1 more source

