Tomida A, Tsuruo T
Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan.
Anticancer Drug Des. 1999 Apr;14(2):169-77.
Most solid tumors show resistance to current chemotherapy. This drug resistance can be associated with the unique physiology of solid tumors. Solid tumors generally have regions of low oxygen (hypoxia), low pH and low levels of glucose, which are not observed in normal tissues. These tumor-specific conditions commonly cause the glucose-regulated stress response of cancer cells. Accumulating evidence shows that the stress response leads to induction of resistance to multiple drugs, such as etoposide, doxorubicin, camptothecin and vincristine. This type of drug resistance is reversible and decays rapidly when stress conditions are removed. The induction of drug resistance can be partly explained by cell cycle arrest at the G1 phase in stressed cells because most anticancer drugs are primarily effective against rapidly dividing cells. Specific mechanisms, such as the decreased expression of DNA topoisomerase (topo) II alpha for the resistance to topo II poisons, are also involved in the drug resistance. Stressed cells, however, become hypersensitive to cisplatin, one of the most effective drugs against solid tumors, suggesting that preferential cytotoxicity to stressed cells may be important for the clinical efficacy against solid tumors. Further characterization of stressed cells will provide a unique target to circumvent the drug resistance of solid tumors.
大多数实体瘤对当前的化疗表现出耐药性。这种耐药性可能与实体瘤独特的生理学特性有关。实体瘤通常具有低氧(缺氧)、低pH值和低葡萄糖水平的区域,而这些在正常组织中并未观察到。这些肿瘤特异性条件通常会引发癌细胞的葡萄糖调节应激反应。越来越多的证据表明,这种应激反应会导致对多种药物产生耐药性,如依托泊苷、阿霉素、喜树碱和长春新碱。这种类型的耐药性是可逆的,当应激条件消除时会迅速衰减。耐药性的诱导部分可以通过应激细胞在G1期的细胞周期停滞来解释,因为大多数抗癌药物主要对快速分裂的细胞有效。特定机制,如对拓扑异构酶(topo)IIα表达降低以抵抗topo II毒药,也与耐药性有关。然而,应激细胞对顺铂变得高度敏感,顺铂是治疗实体瘤最有效的药物之一,这表明对应激细胞的优先细胞毒性可能对实体瘤的临床疗效很重要。对应激细胞的进一步表征将为克服实体瘤的耐药性提供一个独特的靶点。