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首页> 外文期刊>British Journal of Cancer >Novel SMAC-mimetics synergistically stimulate melanoma cell death in combination with TRAIL and Bortezomib
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Novel SMAC-mimetics synergistically stimulate melanoma cell death in combination with TRAIL and Bortezomib

机译:新型SMAC模拟物与TRAIL和Bortezomib协同增效刺激黑色素瘤细胞死亡

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摘要

Background:XIAP (X-linked inhibitor of apoptosis protein) is an anti-apoptotic protein exerting its activity by binding and suppressing caspases. As XIAP is overexpressed in several tumours, in which it apparently contributes to chemoresistance, and because its activity in vivo is antagonised by second mitochondria-derived activator of caspase (SMAC)/direct inhibitor of apoptosis-binding protein with low pI, small molecules mimicking SMAC (so called SMAC-mimetics) can potentially overcome tumour resistance by promoting apoptosis.
机译:背景:XIAP(X连锁凋亡蛋白抑制剂)是一种抗凋亡蛋白,通过结合和抑制胱天蛋白酶发挥其活性。由于XIAP在几种肿瘤中过表达,显然在其中促进了化学抗性,并且由于其体内活性被第二个线粒体衍生的半胱天冬酶(SMAC)激活剂/具有低pI的凋亡结合蛋白直接抑制剂所拮抗,因此小分子模拟SMAC(所谓的SMAC模拟物)可以通过促进细胞凋亡来克服肿瘤抵抗力。

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