CETSA® For Navigating the Chemistry and Exploring the Biology of Protein Degraders
CETSA®, a patented technology by Pelago Bioscience, is a well-established label-free technology that can be used to assess protein-ligand interactions in the native cellular environment of both the POI and the E3 ligase. The CETSA® Navigate HT platform enables robust and sensitive confirmation of target engagement (TE). With the same detection format, it is possible to simultaneously monitor the resulting PROTAC-mediated POI degradation. With the unbiased proteome-wide format CETSA® Explore, further insights can be generated on the mechanism of action of degraders.
- Targeted protein degradation is an emerging therapeutic modality and there is a growing appreciation for PROTACs as chemical probes for target identification and validation.
- CETSA® Navigate HT allows the validation of target engagement and the quantification of physiologically relevant potency in live cells, leveraging on AlphaLISA® SureFire® Ultra™ detection solutions.
- The CETSA® Explore format enables further insight into the mechanism of action of PROTACs.