Webinar Overview: This webinar is intended for those interested in learning about how the ubiquitin-proteasome system (UPS) can be exploited for .. Read more inducing targeted protein degradation, and for those who are working on developing proteolysis-targeting chimeric molecules (PROTACs) and other molecular degraders. The webinar will discuss mechanistic biochemistry and pharmacology of the UPS and the E3 ligases involved; will highlight some of the assays and technologies available to study the pathways and interactions; and offer insights on how to design and optimize degrader molecules. Details to be discussed in the talks are given below. Insights into Protein Degradation and Pharmacodynamic Predictions Stewart Fisher, PhD, Chief Scientific Officer, C4 Therapeutics Targeted protein degradation, a transformative new drug discovery approach, utilizes small molecule degraders to leverage the cellular protein recycling machinery to induce target protein destruction. Specifically, these degraders act as catalytic activators for an E3 ligase to initiate target protein ubiquitination, and the subsequent ubiquitinated target protein is recognized by the cellular proteasome for degradation. This talk will discuss the application of an enzymology framework to characterize cellular degradation data and the extension of these insights to pharmacodynamic modeling and predictions.
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