Thomas Roux1, Thomas Raebiger2,Markus Schappacher2 Stefan Kiefer2, Najim Douayry1, Fanny Plénière1, François Degorce1 and Eric Trinquet1.
1Cisbio Bioassays, Codolet, France I 2BMG LABTECH GmbH, Ortenberg, Germany
Epigenetics and G Protein Coupled Receptors (GPCR) are two important target families in the drug discovery field. On the one hand bromodomain modules, so called epigenetic readers, that bind histone acetyl moieties and play an important role in gene transcription regulation processes have been recently shown as potential druggable targets for cancer therapies, among others. In addition, the role of GPCR in various diseases and the interest of finding drugs targeting these proteins no longer need to be demonstrated.
High-throughput screening to assess these targets requires both robust and reliable assays and instrumentation. Particularly BMG LABTECH has recently introduced the new PHERAstar FSX High Throughput Screening microplate reader. The new TRF Laser in the PHERAstar FSX enables faster reading combined with higher performance. In this study, two HTRF assays were selected to highlight the improved performances of the new PHERAstar FSX microplate reader.
HTRF® assays for epigenetic and GPCRs, such as second messenger assessment, have been demonstrated to be a robust and user friendly platform for target based screening. The results obtained during the present evaluation show that the combination of these assays with the use of PHERAstar FSX provide a superior solution for ultra high throughput screening.