EGFR-TKI resistance in NSCLC patients: mechanisms and strategies.

摘要: The epidermal growth factor receptor (EGFR) is a kind of tyrosine kinase (RTK) that plays critical role in the initiation and development malignant tumors via modulating downstream signaling pathways. In non-small cell lung cancer (NSCLC), activating mutations located domains EGFR have been demonstrated multiple researches as "Achilles' heel" this deadly disease since they could be well-targeted by inhibitors (EGFR-TKIs). However, it's still too early to celebrate first-generation EGFR-TKIs such gefitinib erlotinib only achieved limited clinical benefits acquired resistance drugs occurred inevitably almost all NSCLC patients. order make most develop more effective regimens for patients, researchers majoring different aspects start battle against EGFR-TKI resistance. Challenging it is, we progress stably step firmly toward final victory. This review will summarize major mechanisms EGFR-TKIs, then discuss rationally designed molecular target accordance with each mechanism, hope shedding light on great achievements obtained tough obstacles overcome disease.