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A selective inhibitor of the immunoproteasome subunit LMP2 induces apoptosis in PC-3 cells and suppresses tumour growth in nude mice

机译:免疫蛋白酶体亚基LMP2的选择性抑制剂诱导PC-3细胞凋亡并抑制裸鼠的肿瘤生长

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摘要

Background: Although the proteasome is a validated anticancer target, the clinical application of its inhibitors has been limited because of inherent systemic toxicity. To broaden clinical utility of proteasome inhibitors as anticancer agents, it is critical to develop strategies to selectively target proteasomes in cancer cells. The immunoproteasome is an alternative form of the constitutive proteasome that is expressed at high levels in cancer tissues, but not in most normal cells in the body.
机译:背景:尽管蛋白酶体是经过验证的抗癌靶标,但由于其固有的全身毒性,其抑制剂的临床应用受到了限制。为了扩大蛋白酶体抑制剂作为抗癌剂的临床应用,开发在癌细胞中选择性靶向蛋白酶体的策略至关重要。免疫蛋白酶体是组成型蛋白酶体的替代形式,其在癌症组织中高水平表达,但在体内大多数正常细胞中不表达。

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