小分子酪氨酸激酶抑制剂耐药机制

表皮生长因子受体（epidermal growth factor receptor，EGFR）通路异常在肿瘤发生、发展过程中起到非常重要的作用，特异性抑制该通路的小分子受体酪氨酸激酶抑制剂在肿瘤治疗上取得了显著的效果，但是该药在临床上已经出现耐药现象，现将有关EGFR基因突变、EGFR旁路信号通路的激活、下游信号分子的结构性活化3个方面对EGFR抑制剂耐药机制的研究进展进行综述。

Drug Resistant Mechanism of Small Molecular Tyrosine Kinase Inhibitors

The epidermal growth factor receptor （EGFR） pathway plays an important role in tumor formation and development. Small molecular receptor tyrosine kinase inhibitors specifically inhibiting EGFR pathway have displayed significant effectiveness in cancer therapy. However, drug resistance against the kinase inhibitors has already emerged as problems in clinical. This review summarizes the latest researches on the mechanisms of drug resistance to EGFR inhibitors, including EGFR mutations, activation of EGFR alternative pathways and structural activation of signaling molecules downstream EGFR pathway.