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下一代蛋白酶体抑制剂卡非佐米和奥普佐米通过诱导未折叠蛋白反应和 ATF4 激活促生存自噬。

The next generation proteasome inhibitors carfilzomib and oprozomib activate prosurvival autophagy via induction of the unfolded protein response and ATF4.

机构信息

Department of Medicine, University of Pittsburgh, University of Pittsburgh Cancer Institute, Pittsburgh, PA, USA.

出版信息

Autophagy. 2012 Dec;8(12):1873-4. doi: 10.4161/auto.22185. Epub 2012 Sep 20.

Abstract

The proteasome inhibitor bortezomib has shown remarkable clinical success in the treatment of multiple myeloma. However, the efficacy and mechanism of action of bortezomib in solid tumor malignancies is less well understood. In addition, the use of this first-in-class proteasome inhibitor is limited by several factors, including off-target effects that lead to adverse toxicities. We recently reported the impact and mechanisms of carfilzomib and oprozomib, second-in-class proteasome inhibitors with higher specificities and reduced toxicities, against head and neck squamous cell carcinoma (HNSCC). Carfilzomib and oprozomib potently inhibit HNSCC cell survival and the growth of HNSCC tumors. Both compounds promote upregulation of proapoptotic BIK and antiapoptotic MCL1, which serves to mediate and attenuate, respectively, the killing activities of these proteasome inhibitors. Both compounds also induce complete autophagic flux that is partially dependent on activation of the unfolded protein response (UPR) and upregulation of ATF4. Carfilzomib- and oprozomib-induced autophagy acts to promote HNSCC cell survival. Our study indicates that the therapeutic benefit of these promising proteasome inhibitors may be improved by inhibiting MCL1 expression or autophagy.

摘要

蛋白酶体抑制剂硼替佐米在多发性骨髓瘤的治疗中显示出显著的临床疗效。然而,硼替佐米在实体瘤恶性肿瘤中的疗效和作用机制还不太清楚。此外,由于存在导致不良反应的脱靶效应等因素,这种首创的蛋白酶体抑制剂的应用受到限制。我们最近报道了第二代蛋白酶体抑制剂卡非佐米和奥普佐米对头颈部鳞状细胞癌(HNSCC)的影响和作用机制。卡非佐米和奥普佐米能有效抑制 HNSCC 细胞的存活和 HNSCC 肿瘤的生长。这两种化合物都能促进促凋亡 BIK 和抗凋亡 MCL1 的上调,分别介导和减弱这些蛋白酶体抑制剂的杀伤活性。这两种化合物还诱导完全自噬通量,部分依赖未折叠蛋白反应(UPR)的激活和 ATF4 的上调。卡非佐米和奥普佐米诱导的自噬作用促进 HNSCC 细胞的存活。我们的研究表明,通过抑制 MCL1 表达或自噬,这些有前途的蛋白酶体抑制剂的治疗益处可能会得到改善。

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