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.
A Real-Time Annexin V Method for Monitoring Programmed Cell DeathPoster
The RealTime-Glo™ Annexin V Apoptosis and Necrosis Assay detects the kinetics of apoptosis and secondary necrosis in real time resulting from a variety of treatments (including biologics) to induce cell deathREAD MORE
Preclinical drug screening in new generation Alzheimer’s disease mouse models: The MODEL-AD Consortium StrategyPoster
A brief overview of the Preclinical Testing Core of the MODEL-AD consortium.READ MORE
Exploiting Polypharmacology in Precision Oncology: Identification of Differential Kinase Off-targets Among Clinical PARP InhibitorsPoster
Can we use computational methods to identify previously unknown off-targets of PARP inhibitors that can explain their observed differences?READ MORE