A short overview of dual targeting HDAC inhibitors
Dec 8, 2024 · Histone deacetylases (HDACs) are enzymes that interact with histone acetyltransferases (HATs) to remove acetyl groups from lysine residues, thereby maintaining …
Slow-Binding and Covalent HDAC Inhibition: A New Paradigm?
Oct 31, 2024 · We identified HDAC inhibitors unable to bind recombinant human HDAC4 while showing inhibition in a typical HDAC4 enzymic assay, suggesting that the obsd. activity rather …
Surface plasmon resonance (SPR) is a well-established optical …
Surface plasmon resonance (SPR) is a well-established optical biosensor technology numerous proven applications in the analysis of molecular connections as well such as surface area and …
Overlapping and non-overlapping roles of the class-I histone ...
Our findings suggest that the class-I HDAC-1 corepressors LET-418, SIN-3, and SPR-1 may cooperatively regulate the expression levels of some genes during C. elegans embryogenesis …
An Inhibitor of GSK3B and HDACs Kills Pancreatic Cancer Cells and …
In studies of PDAC cells and 2 mouse models of PDAC, we found a dual inhibitor of GSK3B and HDACS (metavert) to induce cancer cell apoptosis, reduce migration and expression of stem …
Natural Compound Histone Deacetylase Inhibitors (HDACi): …
To treat a multifactorial disease such as cancer, a combination treatment strategy seems to be the best approach. Here we focus on natural histone deacetylase inhibitors (HDACi), their clinical …
HDAC Inhibitors: Innovative Strategies for Their Design and ...
In this review, we will focus on the recent advances and latest discoveries of innovative strategies in the development and applications of compounds that demonstrate inhibitory or degradation …
Tubulin/HDAC dual-target inhibitors: Insights from design …
Jan 5, 2025 · At present, tubulin/HDAC dual-target inhibitors have been obtained in three main ways: uncleavable linked pharmacophores, cleavable linked pharmacophores, and …
HDAC inhibition imparts beneficial transgenerational effects in ...
Dec 17, 2014 · We demonstrate that histone deacetylase (HDAC) inhibition can elicit changes in DNA methylation in Huntington’s disease (HD) human fibroblasts, as well as in sperm from HD …
HDAC inhibitors improve CRISPR-mediated HDR editing efficiency …
Among the six HDAC inhibitors we examined, vorinostat, or suberoylanilide hydroxamic acid (SAHA), led to the highest HDR efficiency at both open and closed loci, with acceptable toxicity.