Assessing the Suitability of Deubiquitylases As Substrates For Targeted Protein Degradation

Abstract excerpt

<h4>Summary</h4> The development of selective inhibitors of Deubiquitylase enzymes (DUBs) is difficult due to a high level of homology in the active sites of the ≈ 100 such enzymes in the human proteome. A potential way to achieve this in a more facile manner would be to develop PROTACs or molecular glues that engage the target DUB in a less conserved region outside of the catalytic domain. However, this raises t...

Topics

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• Endopeptidases
• Hydrolysis
• Mutation
• Neoplasms
• Protein Degradation and Inhibitors
• Ubiquitin
• Ubiquitin and proteasome pathways
• von Hippel-Lindau Disease

Identifiers and source

Literature Corpus work

cb085893-ba75-55f6-8a3f-3a128a80b18a

DOI

10.1101/2025.06.13.659525