Enabling Epigenetics Studies from HTS to SAR : A Novel HTRF® Platform to Identify and Characterize Reader Domain Inhibitors
Poster Oct 10, 2014
T. Roux1, M. Badol1, N. Douayry1, L. Sergeant1, E.Trinquet1, F. Degorce1, S. Milhas2, S. Betzi2, C. Derviaux2, C. Eydoux3, J. Letienne2, A. Lugari2, Y. Collette2, J-C. Guillemot3 et X. Morelli2
Over recent years, significant drug discovery efforts have been made to identify potent and selective inhibitors of epigenetic targets. Proteins of this target class are classified into readers, writers and erasers of marks on histones or other nuclear proteins and DNA. By regulating a combination of posttranslational marks, they tightly control gene expression. Their deregulation has been linked to the development of various diseases, particularly in oncology.
Here we describe a novel assay platform based on the HTRF technology which enables the discovery and the characterization of novel reader domain inhibitors. More than 20 different assays have been built up to monitor the interaction of Bromodomain, Tudor domains, MBT domains and Chromodomains with histone peptides.