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CETSA® For Navigating the Chemistry and Exploring the Biology of Protein Degraders

INTRODUCTION

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.

Key Learnings

  • 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.
EFMC-ACSMEDI23_FR

Download our poster and explore the biology of protein degraders.

Publications

  1. Martinez Molina, D. et al. Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay. Science 341, 84-87 (2013)
  2. Chernobrovkin at al., SLAS Discovery 2021, DOI: 10.1177/2472555220984372

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