Department of Cell Biology and Genetics, Faculty of Science, Palacky University, Slechtitelu 11, 78371 Olomouc, Czech Republic.
Curr Pharm Des. 2011;17(15):1483-99. doi: 10.2174/138161211796197124.
Proteasome inhibition is a modern and surprisingly successful approach how to cancer treatment. Bortezomib (Velcade®) is a first-in-class proteasome inhibitor and has been approved for first-line treatment of multiple myeloma and second-line treatment of mantle cell lymphoma. There have been almost 200 clinical trials with bortezomib, both as a single agent and in combination with other drugs, for various cancers, as listed in the US National Cancer Institute database. However, bortezomib's mechanism of action remains elusive despite enormous progress in our knowledge of the cell biology of the ubiquitin-proteasome system (UPS) and bortezomib-induced signaling events in cancer cells. This review maps a rapidly growing and open body of research in both areas.
蛋白酶体抑制是一种现代的、令人惊讶的成功的癌症治疗方法。硼替佐米（万珂®）是一种首创的蛋白酶体抑制剂，已被批准用于多发性骨髓瘤的一线治疗和套细胞淋巴瘤的二线治疗。在美国国家癌症研究所数据库中列出，硼替佐米已经进行了近 200 项临床试验，无论是作为单一药物还是与其他药物联合使用，都用于各种癌症。然而，尽管我们对泛素-蛋白酶体系统（UPS）的细胞生物学和硼替佐米诱导的癌细胞信号事件有了巨大的认识进展，但硼替佐米的作用机制仍然难以捉摸。这篇综述描绘了这两个领域中快速发展和开放的研究领域。
