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Targeting the ubiquitin-proteasome system for cancer therapy

机译：靶向泛素-蛋白酶体系统进行癌症治疗

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Introduction: The ubiquitin-proteasome system (UPS) degrades 80-90% of intracellular proteins. Cancer cells take advantage of the UPS for their increased growth and decreased apoptotic cell death. Thus, the components that make up the UPS represent a diverse group of potential anti-cancer targets. The success of the first-in-class proteasome inhibitor bortezomib not only proved that the proteasome is a feasible and valuable anti-cancer target, but also inspired researchers to extensively explore other potential targets of this pathway. Areas covered: This review provides a broad overview of the UPS and its role in supporting cancer development and progression, especially in aspects of p53 inactivation, p27 turnover and NF-κB activation. Also, efforts toward the development of small molecule inhibitors (SMIs) targeting different steps in this pathway for cancer treatment are reviewed and discussed. Expert opinion: Whereas some of the targets in the UPS, such as the 20S proteasome, Nedd8 activating enzyme and HDM2, have been well-established and validated, there remains a large pool of candidates waiting to be investigated. Development of SMIs targeting the UPS has been largely facilitated by state-of-the-art technologies such as high-throughput screening and computer-assisted drug design, both of which require a better understanding of the targets of interest.
机译：简介：泛素-蛋白酶体系统（UPS）降解80-90％的细胞内蛋白质。癌细胞利用UPS来增加其生长并减少凋亡细胞死亡。因此，组成UPS的组件代表了各种各样的潜在抗癌目标。一流的蛋白酶体抑制剂硼替佐米的成功不仅证明了蛋白酶体是可行且有价值的抗癌靶标，还激发了研究人员广泛探索该途径的其他潜在靶标。涵盖的领域：这篇综述广泛概述了UPS及其在支持癌症发展和进展中的作用，特别是在p53失活，p27转换和NF-κB激活方面。此外，对开发针对小分子抑制剂（SMIs）的努力进行了审查和讨论，该小分子抑制剂针对该癌症治疗途径中的不同步骤。专家意见：尽管UPS中的某些目标（例如20S蛋白酶体，Nedd8活化酶和HDM2）已经得到了充分确立和验证，但仍有大量候选对象等待调查。诸如UPS的高通量筛选和计算机辅助药物设计等最新技术在很大程度上促进了针对UPS的SMI的开发，这两项都需要对目标物有更好的了解。

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