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Targeting ubiquitination for cancer therapies

机译：靶向泛素化治疗癌症

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摘要

Ubiquitination, the structured degradation and turnover of cellular proteins, is regulated by the ubiquitin-proteasome system (UPS). Most proteins that are critical for cellular regulations and functions are targets of the process. Ubiquitination is comprised of a sequence of three enzymatic steps, and aberrations in the pathway can lead to tumor development and progression as observed in many cancer types. Recent evidence indicates that targeting the UPS is effective for certain cancer treatment, but many more potential targets might have been previously overlooked. In this review, we will discuss the current state of small molecules that target various elements of ubiquitination. Special attention will be given to novel inhibitors of E3 ubiquitin ligases, especially those in the SCF family.
机译：泛素化，细胞蛋白的结构化降解和周转受泛素-蛋白酶体系统（UPS）调控。对于细胞调节和功能至关重要的大多数蛋白质都是该过程的目标。泛素化由三个酶促步骤组成，正如许多癌症类型中所观察到的，该途径中的异常可导致肿瘤的发生和发展。最近的证据表明，以UPS为目标对某些癌症治疗有效，但是以前可能忽略了许多其他潜在目标。在这篇综述中，我们将讨论靶向泛素化各种元素的小分子的现状。将特别关注E3泛素连接酶的新型抑制剂，尤其是SCF家族的抑制剂。

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