Histone deacetylase inhibitors: Isoform selectivity improves survival in a hemorrhagic shock model

Histone Deacetylase Inhibitors: Structure-Based Modeling and Isoform-Selectivity Prediction

An enhanced version of comparative binding energy (COMBINE) analysis, named COMBINEr, based on both ligand-based and structure-based alignments has been used to build several 3-D QSAR models for the eleven human zinc-based histone deacetylases (HDACs). When faced with an abundance of data from diverse structure-activity sources, choosing the best paradigm for an integrative analysis is difficul...

Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.

The human HDAC (histone deacetylase) family, a well-validated anticancer target, plays a key role in the control of gene expression through regulation of transcription. While HDACs can be subdivided into three main classes, the class I, class II and class III HDACs (sirtuins), it is presently unclear whether inhibiting multiple HDACs using pan-HDAC inhibitors, or targeting specific isoforms tha...

Combination of isoform-selective histone/protein deacetylase inhibitors improves Foxp3+ T-regulatory cell function

Comment on: Beier UH, et al. Sci Signal 2012; 5:ra45.

a structure–activity relationship survey of histone deacetylase (hdac) inhibitors

Butyrate Histone Deacetylase Inhibitors

In addition to being a part of the metabolic fatty acid fuel cycle, butyrate is also capable of inducing growth arrest in a variety of normal cell types and senescence-like phenotypes in gynecological cancer cells, inhibiting DNA synthesis and cell growth in colonic tumor cell lines, suppressing hTERT mRNA expression and telomerase activity in human prostate cancer cells, and inducing stem cell...