Drug-target engagement technologies are essential to the successful progression of pharmaceutical research because they support target validation, molecular pharmacology and pharmacokinetic-pharmacodynamic (PKPD) studies. Novel methods will be presented that enable the measurement of binding site engagement of the E3 ubiquitin ligase component protein cereblon, the therapeutically relevant target of the immunomodulatory drugs (IMiDs) such as thalidomide and certain proteolysis targeted chimeras (PROTACs). In-cell occupancy assays were used to understand the relationships between physicochemistry, pharmacology, and cellular bioavailability of small molecule modulators. Biophysical cereblon assays will also be described that reveal deeper insights into molecular modes-of-action that will advance the field of targeted protein degradation.

Assessing cereblon engagement by targeted protein degraders

Fall 2022 abstracts, posters, and presentations will launch in mid-September.

ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.