Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands.
Proteolysis targeting chimeras (PROTACs) hijacking the cereblon (CRBN) E3 ubiquitin ligase have emerged as a novel paradigm in drug development. Herein we found that linker attachment points of CRBN ligands highly affect their aqueous stability and neosubstrate degradation features. This work provides a blueprint for the assembly of future heterodimeric ... CRBN-based degraders with tailored properties.
ACS Med Chem Lett
Date: Nov. 11, 2021
PubMed ID: 34795861
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