Article

Tuning the open-close equilibrium of Cereblon with small molecules influences protein degradation

2025-12-22

Abstract excerpt

Most PROTACs and molecular glue degraders currently approved or in clinical trials recruit Cereblon (CRBN) as the ubiquitin E3 ligase. Upon binding ligands and molecular glues, CRBN undergoes a significant structural rearrangement from an open to closed state, defined by the positioning of the thalidomide-binding domain (TBD) with respect to the Lon domain. However, the exact molecular basis for this ligand-induce...

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Literature Corpus work: 0171e6c5-093d-5745-a37c-b6c968a71328
DOI: 10.64898/2025.12.19.695617

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