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Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2021-10-18 , DOI: 10.1021/acsmedchemlett.1c00368 Aleša Bricelj 1 , Yuen Lam Dora Ng 2 , Dominic Ferber 3 , Robert Kuchta 3 , Sina Müller 2 , Marius Monschke 4 , Karl G Wagner 4 , Jan Krönke 2 , Izidor Sosič 1 , Michael Gütschow 3 , Christian Steinebach 3
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2021-10-18 , DOI: 10.1021/acsmedchemlett.1c00368 Aleša Bricelj 1 , Yuen Lam Dora Ng 2 , Dominic Ferber 3 , Robert Kuchta 3 , Sina Müller 2 , Marius Monschke 4 , Karl G Wagner 4 , Jan Krönke 2 , Izidor Sosič 1 , Michael Gütschow 3 , Christian Steinebach 3
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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.
中文翻译：
连接体附着点对 Cereblon 配体稳定性和新底物降解的影响
劫持 cereblon (CRBN) E3 泛素连接酶的蛋白水解靶向嵌合体 (PROTAC) 已成为药物开发的新范例。在此，我们发现 CRBN 配体的连接基附着点极大地影响其水稳定性和新底物降解特征。这项工作为未来组装具有定制特性的基于异二聚 CRBN 的降解剂提供了蓝图。
更新日期：2021-11-11
中文翻译：
连接体附着点对 Cereblon 配体稳定性和新底物降解的影响
劫持 cereblon (CRBN) E3 泛素连接酶的蛋白水解靶向嵌合体 (PROTAC) 已成为药物开发的新范例。在此，我们发现 CRBN 配体的连接基附着点极大地影响其水稳定性和新底物降解特征。这项工作为未来组装具有定制特性的基于异二聚 CRBN 的降解剂提供了蓝图。
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