Webinar I May 14, 2024
This is the fourth episode of our second 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, we discuss data from a recent preprint on the kinetic analysis of Proteolysis-targeting chimeras (PROTACs). PROTACs and molecular glues are novel pharmaceutical compounds inducing the degradation of a target protein. This mode of action depends on the formation of a ternary complex with two proteins. Ternary complexes are influenced by complex cooperativity and avidity effects, which makes the kinetic characterization challenging. You will learn how to simultaneously measure binary and ternary interaction kinetics in high throughput using a proximity binding assay with a Y-shaped DNA nanostructure. The assay is applied to cereblon and von Hippel-Lindau as E3 ligase substrate receptors. We will showcase results from a screening of a range of compounds and demonstrate how real-time kinetics elucidate differences that cannot be dissected by affinity alone.
If you are interested in another application, you can find all future episodes of this webinar series here.