A Live Cell Target Engagement Method for Intractable Protein Complexes (#31)
Matthew Robers
1
- Promega Corporation, Madison, WI, United States
- We present a novel configuration of the NanoBRET method that conditionally measures drug engagement at protein complexes
- Paralog selectivity at individual RAF protomers exposes a drug escape mechanism within the RAS-RAF signalosome
- A KRAS BRET probe exposes novel vulnerability at the KRAS switch-2 pocket
- Enabling Target 2035: Bespoke BRET probes can be generated using DNA Encoded Library Chemistry