Receptor Tyrosine Kinases (RTKs) regulate many critical processes such as cell growth, differentiation, and survival through the recruitment of intracellular signaling molecules. Dysregulated RTK activity can affect many cellular functions, often culminating in cancer, making RTKs prime targets for new anti-cancer agents. However, the efficacy of several of these drugs is limited by the development of drug-induced adverse events. Furthermore, mutations in RTKs may alter receptor activity or prevent drug binding as a consequence of more complex cellular mechanisms (i.e., alteration of receptor subcellular localization, and signaling/trafficking kinetics). Many of the methodologies currently used to study RTK activation and screen for therapeutics revolve around RTK kinase activity. However, kinase activity-based assays are limited in throughput and overlook additional key determinants of ligand therapeutic efficacy, including kinetics, localization, and functional selectivity. The development of tools providing new insight into these complex mechanisms is crucial to better understand RTK biology and to develop more effective RTK-targeting drugs.
In this GEN webinar, our expert panelists will introduce bioSensAll™, an enhanced bystander bioluminescence resonance energy transfer (ebBRET)-based biosensor technology and its applications to interrogate RTK biology and expand current RTK drug discovery efforts. Using examples of different RTKs, our presenters will describe a unique set of biosensors spanning different effectors that allows for the real-time mapping and spatiotemporal monitoring of the signal transduction pathways engaged upon activation of RTKs and their mutated variants, in different cellular compartments. This new technology offers a new pluridimensional view of RTK signaling, enabling advancements in RTK-targeting drug discovery.
A live Q&A session will follow the presentations, offering you a chance to pose questions to our expert panelists.