Which is a histone deacetylase inhibitor?
Histone deacetylase (HDAC) inhibitors are a relatively new class of anti-cancer agents that play important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis, and cell cycle arrest in cancer cells.
How does butyrate inhibit HDAC?
Butyrate is a SCFA known to act as a histone deacetylase inhibitor (HDACi), favoring histone acetylation and thus remodeling of chromatin towards an open and transcriptionally competent state3.
Is valproic acid an HDAC inhibitor?
Thus, HDAC inhibitors are candidate drugs for differentiation therapy of cancer. Here, we show that the well-tolerated antiepileptic drug valproic acid is a powerful HDAC inhibitor. Valproic acid relieves HDAC-dependent transcriptional repression and causes hyperacetylation of histones in cultured cells and in vivo.
Do HDAC inhibitors increase transcription?
HDACIs repress transcription by blocking elongation, as we have shown previously in human breast cancer (BT474) and non-cancerous breast epithelial (MCF10A) cell lines using GRO-seq (Kim et al., 2013).
How does valproic acid inhibit HDAC?
Valproic acid relieves HDAC-dependent transcriptional repression and causes hyperacetylation of histones in cultured cells and in vivo. Valproic acid inhibits HDAC activity in vitro, most probably by binding to the catalytic center of HDACs.
Is butyrate a HDAC inhibitor?
Sodium butyrate (NaB) is a histone deacetylase (HDAC) inhibitor exhibiting anti-inflammatory and neuroprotective effects in a rat ischemic model of stroke as well as a myocardial ischemia model.
Is valproic acid histone deacetylase inhibitor?
Valproic acid, however, acts through a distinct pathway that involves direct inhibition of histone deacetylase (IC50 for HDAC1 = 0.4 mm). At therapeutic levels, valproic acid mimics the histone deacetylase inhibitor trichostatin A, causing hyperacetylation of histones in cultured cells.
Is valproic acid a HDAC inhibitor?
What is the difference between butyrate and beta hydroxybutyrate?
Chemically, BOHB is almost identical to butyrate with the exception of one added oxygen. Both butyrate and BOHB can be used by mitochondria as an efficient fuel, and both have anti-inflammatory and epigenetic effects. However, in this inflammation-modulating role, BOHB is more potent².