State Key Laboratory of Oncology in South China, Guangdong Esophageal Cancer Institute; Cancer Center, Sun Yat-sen University Cancer Center, Guangzhou, 510060, China.
Mol Cancer. 2018 Feb 19;17(1):25. doi: 10.1186/s12943-018-0775-3.
Multidrug resistance (MDR) triggered by ATP binding cassette (ABC) transporter such as ABCB1, ABCC1, ABCG2 limited successful cancer chemotherapy. Unfortunately, no commercial available MDR modulator approved by FDA was used in clinic. Tyrosine kinase inhibitors (TKIs) have been administrated to fight against cancer for decades. Almost TKI was used alone in clinic. However, drug combinations acting synergistically to kill cancer cells have become increasingly important in cancer chemotherapy as an approach for the recurrent resistant disease. Here, we summarize the effect of TKIs on enhancing the efficacy of conventional chemotherapeutic drug in ABC transporter-mediated MDR cancer cells, which encourage to further discuss and study in clinic.
多药耐药（MDR）由 ATP 结合盒（ABC）转运蛋白触发，如 ABCB1、ABCC1、ABCG2，限制了癌症化疗的成功。不幸的是，没有 FDA 批准的商业 MDR 调节剂在临床上使用。酪氨酸激酶抑制剂（TKIs）已用于对抗癌症数十年。几乎所有 TKI 都单独用于临床。然而，协同作用杀死癌细胞的药物组合在癌症化疗中变得越来越重要，成为治疗复发性耐药疾病的一种方法。在这里，我们总结了 TKI 对增强 ABC 转运蛋白介导的 MDR 癌细胞中常规化疗药物疗效的影响，这鼓励我们进一步在临床上进行讨论和研究。
