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Targeting the Interaction of NRF2 and β-TrCP with Molecular Glues
ACS Chemical Biology 2026
Daniel H. O Donovan, Jon Winter-Holt, Gavin W. Collie, Maria Emanuela Cuomo, David John McGarry, Millie Fox, Bo Kyung Alex Seong, Ursula Grazini, Peter Barton, David Longmire, Andrew Lister, Yong Xu, Hazel Mak, Evelyne J. Barrey, Marta Acebrón-García-de-Eulate, Magdalena Richter, Nisha Peter, Maxime Couturier, Gustavo J. Gutierrez, Ryan Guilbert, Wankyu Lee, Pamela A. Lochhead, Argyrides Argyrou
This study developed molecular glues that strengthen the interaction between the transcription factor NRF2 and its E3 ubiquitin ligase substrate receptor β-TrCP, offering a route to modulate the NRF2 antioxidant pathway. Flow Induced Dispersion Analysis (FIDA), on a Fida 1 instrument, was used to measure the apparent binding affinity (Kd) between a fluorescently labelled NRF2-derived degron peptide and the β-TrCP:SKP1 complex, quantifying how the molecular glue NRX-252114 enhances this interaction by tracking changes in hydrodynamic radius. It is an example of using FIDA to quantify small-molecule–induced changes in protein–protein binding affinity in solution.
