Thomas J. Kodadek

This study evaluates whether deubiquitylases (DUBs) can be effectively degraded by PROTACs, finding that some DUBs are degradable while others resist degradation due to auto-deubiquitylation or poor proteasome substrate properties.

This study shows that adding an imidazopyridinium (IP+) unit to macrocyclic peptides enhances their passive membrane permeability, enabling them to enter cells and inhibit intracellular targets like p53-MDM2.

The paper introduces a functional assay to identify non-inhibitory enzyme ligands from bead-displayed compound libraries, applied to E3 ubiquitin ligases, and discovers a novel ligand for VHL.

This study demonstrates a method to degrade native proteins by directly recruiting them to the proteasome without requiring ubiquitylation.