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Proteolysis targeting chimeras (PROTACs) for epigenetics research.
Current Opinion in Chemical Biology ( IF 7.8 ) Pub Date : 2020-03-05 , DOI: 10.1016/j.cbpa.2020.01.010
Anja Vogelmann 1 , Dina Robaa 2 , Wolfgang Sippl 2 , Manfred Jung 3
Affiliation  

Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules and allow selective protein degradation by addressing the natural ubiquitin proteasome system. As this new strategy of chemically induced protein degradation can serve as a biological tool and provides new possibilities for drug discovery, it has been applied to a variety of targets including (nuclear) receptors, kinases, and epigenetic proteins. A lot of PROTACs have already been designed in the field of epigenetics, and their synthesis and characterization highly contributed to structural optimization and improved mechanistic understanding of these molecules. In this review, we will discuss and summarize recent advances in PROTAC discovery with focus on epigenetic targets.

中文翻译:

针对嵌合体(PROTAC)的蛋白水解用于表观遗传学研究。

靶向嵌合体(PROTAC)的蛋白水解是异双功能分子,可通过处理天然遍在蛋白蛋白酶体系统实现选择性蛋白质降解。由于这种化学诱导蛋白质降解的新策略可以用作生物学工具,并为药物发现提供新的可能性,因此已将其应用于多种靶标,包括(核)受体,激酶和表观遗传蛋白。在表观遗传学领域已经设计了许多PROTAC,它们的合成和表征对结构优化和对这些分子的机械理解有了极大的贡献。在这篇综述中,我们将讨论和总结PROTAC发现的最新进展,重点是表观遗传学目标。
更新日期:2020-03-05
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