Reinstating targeted protein degradation with DCAF1 PROTACs in CRBN PROTAC resistant settings

Abstract excerpt

<h4>ABSTRACT</h4> Targeted protein degradation (TPD) of neo-substrates with proteolysis targeting chimeras (PROTACs) or molecular glues has emerged as a key modality in exploring new biology as well as designing new drug candidates where catalytic inhibition is neither efficacious nor an option. TPD is mediated through harnessing E3 ligases and redirecting them to ubiquitinate de novo target proteins for subsequ...

Topics

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• Acrylamides
• Agammaglobulinaemia Tyrosine Kinase
• Fluorescent Dyes
• Half-Life
• Intracellular Space
• Molecular Dynamics Simulation
• Protein Degradation and Inhibitors
• Ubiquitin and proteasome pathways

Identifiers and source

Literature Corpus work

c05799ba-d494-5059-aa18-594b8b6cc464

DOI

10.1101/2023.04.09.536153