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Targeted protein degradation as a powerful research tool in basic biology and drug target discovery.
Nature Structural & Molecular Biology ( IF 16.8 ) Pub Date : 2020-06-15 , DOI: 10.1038/s41594-020-0438-0
Tao Wu 1, 2 , Hojong Yoon 1, 2 , Yuan Xiong 1, 2 , Sarah E Dixon-Clarke 1, 2 , Radosław P Nowak 1, 2 , Eric S Fischer 1, 2
Affiliation  

Controlled perturbation of protein activity is essential to study protein function in cells and living organisms. Small molecules that hijack the cellular protein ubiquitination machinery to selectively degrade proteins of interest, so-called degraders, have recently emerged as alternatives to selective chemical inhibitors, both as therapeutic modalities and as powerful research tools. These systems offer unprecedented temporal and spatial control over protein function. Here, we review recent developments in this field, with a particular focus on the use of degraders as research tools to interrogate complex biological problems.



中文翻译:

靶向蛋白质降解作为基础生物学和药物靶点发现的强大研究工具。

蛋白质活性的受控扰动对于研究细胞和活生物体中的蛋白质功能至关重要。劫持细胞蛋白质泛素化机制以选择性降解感兴趣蛋白质的小分子(即所谓的降解剂)最近已成为选择性化学抑制剂的替代品,既作为治疗方式,又作为强大的研究工具。这些系统提供了对蛋白质功能前所未有的时间和空间控制。在这里,我们回顾了该领域的最新发展,特别关注使用降解剂作为研究工具来探究复杂的生物问题。

更新日期:2020-06-15
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