NanoBRET™ CRBN and VHL Ternary Complex Assays Technical Manual
Literature # TM615
Targeted degradation via small molecule degraders such as a PROTAC or molecular glue require forming a ternary complex consisting of a target protein, a degrader and E3 ligase component. Ternary complex formation is the first key mechanistic step required to achieve target ubiquitination and degradation via the ubiquitin proteasome pathway. The NanoBRET™ Ternary Complex Assays are designed for live-cell detection of complexes that contain either VHL (von Hippel-Lindau disease tumor suppressor) or CRBN (cereblon) E3 ligase component. These assays can be read in either endpoint or kinetic formats and provide insight into how altering the degradation compound composition affects the formation, stability or both of the ternary complex. The NanoBRET™ Ternary Complex Assays can also be used to deconvolute degradation from other cellular pathways that lead to protein level loss and better understand the mechanism of action.
Printed in USA 3/20.