《生命科学》 2009, 21(3): 412-417

靶向EGFR家族的抗肿瘤药物研究进展

代　梅*，郭建辉

(上海艾力斯医药科技有限公司，上海 201203)

摘　要：摘　要：表皮生长因子受体(EGFR，ErbB)家族在肿瘤的发生、发展中具有重要的作用。很多实体肿瘤中存在EGFR家族受体过表达或异常激活。靶向EGFR家族的抗肿瘤药物研发已经成为一个热点领域，并且成功地应用于临床。靶向EGFR家族的抗肿瘤药物可以分为单克隆抗体和小分子酪氨酸激酶抑制剂两大类。单克隆抗体与受体胞外区结合阻止配体-受体的结合或者阻止配体结合引起的受体活化；而小分子酪氨酸激酶抑制剂则结合于胞内激酶区，抑制激酶自磷酸化和下游信号通路激活。
关键词：EGFR， ErbB；受体酪氨酸激酶；单克隆抗体；小分子酪氨酸激酶抑制剂

EGFR-targeted agents in cancer therapy

DAI Mei*， GUO Jian-hui

(Allist Pharmaceuticals Inc， Shanghai 201203， China)

Abstract: Abstract: Epidermal growth factor receptor (EGFR， ErbB) family plays important roles in human cancers. Over-expression or aberrant activation of EGFR receptors occurs in many solid tumors. Drugs targeting EGFR receptors have already been successfully implicated in clinic and all belong to two categories: monoclonal antibodies and tyrosine kinase inhibitors (TKIs). Monoclonal antibodies combine with the extracellular region and TKIs inhibit the intracellular kinase activation with ATP competitive or uncompetitive way.
Key words: EGFR， ErbB; receptor tyrosine kinase; monoclonal anybodies; TKI