Nikolaus Gunkel, DKFZ, Heidelberg
Histone deacetylases (HDACs) are an important class of epigenetic regulators which are involved in the malignant phenotype of multiple cancers and represent a promising set of drug targets. The clinical limitations of HDAC inhibitor therapy is most likely caused by HDAC1/2/3 mediated toxicity of past and current clinical candidates. Especially in the area of neuroblastoma an emerging concept aims at the selective inhibition of HDAC8 and 10. Although a rational combination of 8/10-activity in one molecule is per se a challenging task, the main obstacle so far for such a project was the lack of a HDAC10 assay. We will present assay validation results based on Promega’s nanoBRET. This technology allows, for the first time, to profile class-selective HDAC inhibitors within one assy format.
