High-Resolution Snapshots of Proteasome Inhibitors In Action Revise Inhibition Paradigms and Inspire Next-Generation Inhibitor Design

Abstract

New high-resolution crystal structures reported by Schrader and colleagues refine our understanding of how peptide epoxyketone anticancer drugs inactivate their target: the human proteasome. These findings provide important clues for the design of next-generation proteasome inhibitor drugs.