Abstract 2678 Target class approach accelerates understanding of DUB ligandability and function

The family of deubiquitylases (DUBs) comprises more than 100 proteases that remove ubiquitin from substrate proteins, thereby playing a central role in protein homeostasis and ubiquitin signaling. DUBs are increasingly implicated in a range of disease states. Concomitant with interest in DUBs in disease, is a need for high quality chemical probes to study DUB mechanism at the molecular level and pharmacologically validate members of the enzyme family as disease targets. I will briefly present the platform my lab has developed to identify and rigorous characterization DUB ligands with diverse mechanisms of activation.