The Development and Application of Biophysical Assays for Evaluating Ternary Complex Formation Induced by Proteolysis Targeting Chimeras (PROTACS)

Wei Jiang; Holly Soutter

doi:10.3791/65718

Characterization of Ternary Complex Formation in PROTACs Using Biophysical Assays

January 12, 2024

Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes (Video) | JoVE

01:09 min

•

Isothermal Titration Calorimetry for Evaluating PROTACS-Induced Ternary Complex Formation (Video) | JoVE

01:16 min

•

Biolayer Interferometry (BLI) for Evaluating PROTACS-Induced Ternary Complex Formation (Video) | JoVE

01:23 min

•

Surface Plasmon Resonance (SPR) for Evaluating PROTACS-Induced Ternary Complex Formation (Video) | JoVE

03:36 min

•

Wei Jiang, Holly Soutter

¹Center for the Development of Therapeutics,The Broad Institute of MIT and Harvard

Summary

Here we describe protocols for the biophysical characterization of ternary complex formation induced by proteolysis targeting chimeras (PROTACS) that involve the ubiquitin ligases Von Hippel-Lindau E3 ligase (VHL) and Cereblon (CRBN). Biophysical methods illustrated herein include surface plasmon resonance (SPR), biolayer interferometry (BLI), and isothermal titration calorimetry (ITC).