(1139-D) The power of combining PROTAC degraders targeting cyclin-dependent kinases (CDK4/CDK6) with AlphaLISA® SureFire® screening technology for the study of cell cycle regulation in oncology
Tuesday, February 6, 2024
2:00 PM – 3:00 PM EST
Location: Exhibit Halls AB
Abstract: The AlphaLISA® SureFire® Ultra™ platform has been successfully used in basic and pre-clinical research as well as in drug discovery programs around the world. The SureFire Ultra assay is a homogeneous bead-based method that can be used for small scale or high throughput screening. This technology has been developed to provide unique assay specificity and sensitivity, becoming a powerful tool to detect proteins either associated to cell membranes or localised in cellular compartments. The portfolio covers a wide range of targets involved in different signalling pathways, including but not limited to apoptosis, neuroscience, autophagy and cell cycle regulation. The dysregulation of the cell cycle and activation of cyclin-dependent kinases (CDK’s) is a hallmark of cancer and has become a key area for the discovery of efficient therapies to prevent tumor progression. This study has been focused on the development and validation of assays to specifically investigate the downstream effects of activators and novel PROTAC degraders targeting CDK4/CDK6 cascade. The results, in agreement with the literature, demonstrate the dramatic changes in Rb phosphorylation levels and its further implications in Cyclin A2 and B1 activation. The data presented here highlight once again the utility of SureFire Ultra technology as a platform of choice for the characterization and validation of high-profile oncology targets and demonstrate its utility for downstream pathway analysis.