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癌症是全世界首要的死因之一。据统计,2008年就有760万人死于癌症,其中有100万人死于肺癌,71%的肺癌死者是由于吸烟所致。表皮生长因子受体(EGFR)为受体酪氨酸激酶家族成员之一,其广泛表达于多种肿瘤(如乳腺癌、头颈癌和卵巢癌)中,故而成为抗癌治疗最具潜力的靶点之一。第1代EGFR抑制剂吉非替尼(gefitinib)和埃罗替尼(erlotinib)已获准用于经其他抗肿瘤药物治疗无效的晚期非小细胞肺癌(NSCLC)患者。
Cancer is one of the leading cause of death in the world. According to statistics, 7.6 million people died of cancer in 2008, of which 1 million died of lung cancer and 71% died of lung cancer due to smoking. Epidermal growth factor receptor (EGFR), a member of the receptor tyrosine kinase family, is widely expressed in a variety of tumors, such as breast, head and neck, and ovarian cancers and has therefore become the most promising target for anti-cancer therapy One of the points. The first generation of EGFR inhibitors, gefitinib and erlotinib, have been approved for use in patients with advanced non-small cell lung cancer (NSCLC) who have failed to respond to other antineoplastic agents.