DISCOVER PROTAC Profiling: From DNA-encoded Library to Cellular Degradation

Описание: This is the sixth episode of our third season of the DISCOVER MOLECULAR INTERACTIONS webinar series. Each month we will talk about cutting-edge drug discovery topics like bispecific antibodies, PROTACs or small molecules targeting RNA. We will show you how to characterize the respective molecular interactions in depth, how to create assays with remarkable biological similarity, low sample consumption, high versatility and exceptional ease-of-use.
In this episode, Renaud Morales from Novalix will showcase a prototypical workflow for PROTAC design and characterization. Binders for the model target BRD4 were identified via a DNA-encoded library screening and PROTAC molecules recruiting the E3 ligase Cereblon were designed. The candidate molecules were screened for their binary binding kinetics using high-throughput Surface Plasmon Resonance. Afterwards, ternary complex formation was validated using switchSENSE and a proximity binding assay. Finally, cell degradation assays were performed and results correlated to the interaction data. The presented workflow offered detailed insights into the specificity and mode of action of different PROTAC constructs, combining ligand discovery, biophysical characterization, and cellular validation and thereby aiding rational drug design.

If you are interested in another application, you can find all future episodes of this webinar series here: https://www.dynamic-biosensors.com/we...