Proteasomes are large, multicatalytic protein complexes that cleave cellular proteins into peptides. There are many distinct forms of proteasomes that differ in catalytically active subunits, regulatory subunits, and associated proteins. Proteasome inhibitors are an important class of drugs for the treatment of multiple myeloma and mantle cell lymphoma, and they are being investigated for other diseases. Bortezomib (Velcade) was the first proteasome inhibitor to be approved by the US Food and Drug Administration. Carfilzomib (Kyprolis) and ixazomib (Ninlaro) have recently been approved, and more drugs are in development. While the primary mechanism of action is inhibition of the proteasome, the downstream events that lead to selective cell death are not entirely clear. Proteasome inhibitors have been found to affect protein turnover but at concentrations that are much higher than those achieved clinically, raising the possibility that some of the effects of proteasome inhibitors are mediated by other mechanisms.

中文翻译：

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蛋白酶体抑制剂药物。

蛋白酶体是大型的多催化蛋白复合物，可将细胞蛋白裂解为肽。有许多不同形式的蛋白酶体，它们的催化活性亚基，调节亚基和相关蛋白质均不同。蛋白酶体抑制剂是治疗多发性骨髓瘤和套细胞淋巴瘤的重要药物，目前正在研究其他疾病。硼替佐米（Velcade）是美国食品和药物管理局批准的首个蛋白酶体抑制剂。Carfilzomib（Kyprolis）和ixazomib（Ninlaro）最近已获批准，并且正在开发更多药物。尽管主要的作用机制是抑制蛋白酶体，但导致选择性细胞死亡的下游事件尚不完全清楚。