Cryo-EM reveals a mechanism of USP1 inhibition through a cryptic binding site

Abstract excerpt

Repair of DNA damage is critical to genomic integrity and frequently disrupted in cancers. USP1, a nucleus-localized deubiquitinase, lies at the interface of multiple DNA repair pathways and is a promising drug target for certain cancers. Although multiple inhibitors of this enzyme, including one in phase I clinical trials, have been established, their binding mode is unknown. Here we use cryo-Electron Microscopy...

Topics

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• BRCA1 Protein
• Oxidation-Reduction
• Oxidative Stress
• Protein Interaction Domains and Motifs
• Protein Processing, Post-Translational
• Structure-Activity Relationship
• Tumor Suppressor Proteins
• Viral-associated cancers and disorders

Identifiers and source

Literature Corpus work

675b6afe-9a2a-567c-8860-3ce766be0eef

DOI

10.1101/2022.04.06.487267