3区 · 医学
Article
作者: Dora Ng, Yuen Lam ; Krönke, Jan ; Kuchta, Robert ; Gütschow, Michael ; Ferber, Dominic ; Müller, Sina ; Bricelj, Aleša ; Wagner, Karl G. ; Steinebach, Christian ; Monschke, Marius ; Sosič, Izidor
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.