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Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2019-11-12 , DOI: 10.1021/acsmedchemlett.9b00425
Philip P Chamberlain 1 , Laura A D'Agostino 1 , J Michael Ellis 1 , Joshua D Hansen 1 , Mary E Matyskiela 1 , Joseph J McDonald 1 , Jennifer R Riggs 1 , Lawrence G Hamann 1
Affiliation  

Many cellular processes and pathways are mediated by the regulation of protein-protein complexes. For example, E3 ubiquitin ligases recruit substrate proteins and transfer a ubiquitin tag to target those proteins for destruction by the proteasome. It has now been shown that this cellular process for protein destruction can be redirected by small molecules in both laboratory and clinical settings. This presents a new paradigm in drug discovery, enabling the rapid removal of target proteins linked to disease. In this Innovations review, we will describe the work done on cereblon as a case study on the different strategies available for targeted protein degradation.

中文翻译:

Cereblon介导的蛋白质降解作为治疗手段的演变。

蛋白质-蛋白质复合物的调节介导许多细胞过程和途径。例如,E3泛素连接酶募集底物蛋白质并转移泛素标签以靶向那些蛋白质以被蛋白酶体破坏。现已显示,在实验室和临床环境中,这种破坏蛋白质的细胞过程都可以被小分子重新定向。这为药物发现提出了新的范例,可以快速去除与疾病相关的靶蛋白。在本创新综述中,我们将描述在大脑中完成的工作,作为针对可用于靶向蛋白质降解的不同策略的案例研究。
更新日期:2019-11-28
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