- Histone modifications caused by HDAC are strongly related to epigenetic regulation of transcription
- HDAC inhibitors (HDIs) are a possible strategy in cancer therapy
- Fluorescent HDAC activity and inhibitor assay was performed on a POLARstar OPTIMA microplate reader from BMG LABTECH
Post-translational histone modifications like acetylation play a pivotal role in the epigenetic regulation of transcription. Catalyzing the latter reaction HDACs affect various cellular processes especially cancerogenesis. Although the mechanism of starting cancerogenesis by epigenetic events is not clearly explained inhibition of HDACs has highlighted as a viable principle in cancer therapy.(1) Inhibition of HDACs results in histone overacetylation that in turn can lead to a controlled cell death (apoptosis). Several HDAC inhibitors (HDIs) are in phase I or II clinical trials, for example suberoylanilide hydroxamic acid (SAHA; ZOLINZA®, Merck). In the last years research focused on the development of selective HDIs. To determine the inhibitory effect fluorogenic assays with recombinant proteins could offer a valuable performance. In this application note, the POLARstar OPTIMA fluorescence microplate reader from BMG LABTECH was used to determine the inhibitor effect of SAHA against HDAC1.