AACR POSTER – Degrader
Enhancing Degrader Research with CETSA®
Unlocking New Insights into Targeted Protein Degradation with CETSA: Revealing Both Target Engagement and Off-Target Effects
In the rapidly evolving field of targeted protein degradation (TPD), understanding the complex mechanisms of PROTACs (Proteolysis-targeting chimeras) is crucial. Our research leverages CETSA (Cellular Thermal Shift Assay) to gain deeper insights into PROTAC efficacy by measuring target engagement and degradation. Using this powerful, label-free technology, we identify direct protein binders and evaluate cellular responses, providing a clearer picture of both degradation and off-target effects.
This study explores the use of CETSA to profile small molecule drugs and PROTACs in intact cells and lysates, revealing essential information on compound selectivity, target engagement, and the underlying biological consequences. By profiling various PROTACs, including their effects on proteins like CDK9 and CRBN, our research demonstrates how CETSA can distinguish between cellular responses driven by degradation and those driven by conventional ligand interactions.
Explore how CETSA is transforming the landscape of drug discovery and protein degradation research, offering new opportunities to optimize PROTACs and other degraders for therapeutic applications.
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