基于表观遗传的摄取型药物转运体表达调控是肿瘤耐药干预的新途径

Epigenetics-based regulation of uptake drug transporter expression is a new approach for cancer drug resistance intervention

肿瘤耐药是临床化疗效果不佳的关键因素,其中药物代谢酶和药物转运体表达异常引起肿瘤细胞中药物浓度下降是导致耐药的重要原因之一。文章从药物代谢酶和转运体与肿瘤耐药、药物表观遗传学与耐药、肾癌耐药的潜在靶标OCT2等方面分析了肿瘤摄取转运体表达异常的机制,提出通过表观遗传机制调节肿瘤细胞中摄取型药物转运体表达是逆转肿瘤耐药的新途径。

Drug resistance is a key factor for poor clinical efficacy of chemotherapy. One of the important reasons for drug resistance is the abnormal expression of drug metabolizing enzymes and drug transporters,which results in the decrease of drug concentration in cancer cells. In this paper,the mechanism of abnormal uptake transporter expression in tumors is analyzed from aspects of drug metabolism enzymes and transporters and tumor drug resistance,drug epigenetics and drug resistance,and potential targets of renal cancer drug resistance,such as OCT2. It is proposed that the regulation of uptake drug transporter expression in tumors by epigenetic mechanism is a new way to reverse drug resistance in tumors.