Department of Pharmacology, University of Colorado School of Medicine, Aurora, CO, USA.
Autophagy. 2012 Feb 1;8(2):200-12. doi: 10.4161/auto.8.2.18554.
Chloroquine (CQ) is a 4-aminoquinoline drug used for the treatment of diverse diseases. It inhibits lysosomal acidification and therefore prevents autophagy by blocking autophagosome fusion and degradation. In cancer treatment, CQ is often used in combination with chemotherapeutic drugs and radiation because it has been shown to enhance the efficacy of tumor cell killing. Since CQ and its derivatives are the only inhibitors of autophagy that are available for use in the clinic, multiple ongoing clinical trials are currently using CQ or hydroxychloroquine (HCQ) for this purpose, either alone, or in combination with other anticancer drugs. Here we show that in the mouse breast cancer cell lines, 67NR and 4T1, autophagy is induced by the DNA damaging agent cisplatin or by drugs that selectively target autophagy regulation, the PtdIns3K inhibitor LY294002, and the mTOR inhibitor rapamycin. In combination with these drugs, CQ sensitized to these treatments, though this effect was more evident with LY294002 and rapamycin treatment. Surprisingly, however, in these experiments CQ sensitization occurred independent of autophagy inhibition, since sensitization was not mimicked by Atg12, Beclin 1 knockdown or bafilomycin treatment, and occurred even in the absence of Atg12. We therefore propose that although CQ might be helpful in combination with cancer therapeutic drugs, its sensitizing effects can occur independently of autophagy inhibition. Consequently, this possibility should be considered in the ongoing clinical trials where CQ or HCQ are used in the treatment of cancer, and caution is warranted when CQ treatment is used in cytotoxic assays in autophagy research.
氯喹(CQ)是一种 4-氨基喹啉药物,用于治疗多种疾病。它通过阻断自噬体融合和降解来抑制溶酶体酸化,从而阻止自噬。在癌症治疗中,CQ 常与化疗药物和放射治疗联合使用,因为它已被证明可以增强肿瘤细胞杀伤的效果。由于 CQ 及其衍生物是临床上唯一可用的自噬抑制剂,因此目前有多项正在进行的临床试验正在单独或与其他抗癌药物联合使用 CQ 或羟氯喹(HCQ)来达到这一目的。在这里,我们发现在小鼠乳腺癌细胞系 67NR 和 4T1 中,DNA 损伤剂顺铂或选择性靶向自噬调节的药物,PtdIns3K 抑制剂 LY294002 和 mTOR 抑制剂雷帕霉素可诱导自噬。与这些药物联合使用时,CQ 可增强这些治疗效果,但与 LY294002 和雷帕霉素治疗相比,这种效果更为明显。然而,令人惊讶的是,在这些实验中,CQ 的增敏作用独立于自噬抑制,因为 Atg12、Beclin 1 敲低或巴弗洛霉素处理并不能模拟增敏作用,并且即使在没有 Atg12 的情况下也会发生增敏作用。因此,我们提出,尽管 CQ 可能有助于与癌症治疗药物联合使用,但它的增敏作用可以独立于自噬抑制而发生。因此,在正在进行的临床试验中使用 CQ 或 HCQ 治疗癌症时,应该考虑到这种可能性,并且在自噬研究中使用 CQ 治疗细胞毒性测定时应谨慎。
Neurosurg Focus. 2014-12
Drug Des Devel Ther. 2016-3-7
Endocr Relat Cancer. 2018-4-10
Naunyn Schmiedebergs Arch Pharmacol. 2025-7-1
Front Pharmacol. 2025-5-15
Front Immunol. 2025-4-3
Cell Regen. 2025-4-10
Naunyn Schmiedebergs Arch Pharmacol. 2025-2-27
Exp Hematol Oncol. 2025-2-1
Proc Natl Acad Sci U S A. 2011-7-11
Genes Dev. 2011-3-15
Clin Cancer Res. 2011-2-15
Cancer Biol Ther. 2011-1-15
Cancer Biol Ther. 2011-1-15