Department of Internal Medicine, University of Nebraska Medical Center, Omaha, 68198-7680, USA.
Cancer Invest. 2010 Jun;28(5):515-25. doi: 10.3109/07357900903476760.
Epidermal growth factor is a 170-kd protein that binds to a specific tyrosine kinase receptor, epidermal growth factor receptor (EGFR), on the cell surface. EGFR function is dysregulated in various malignancies including nonsmall cell lung cancer (NSCLC) leading to activation of several signal transduction pathways including K-RAS, PIK3, and STAT3 and STAT5, that promote cell cycle progression, proliferation, invasion, angiogenesis, and inhibit apoptosis. EGFR overexpression is seen in a majority of cases of NSCLC, but its prognostic role is controversial. EGFR inhibitors currently undergoing clinical trials in NSCLC include monoclonal antibodies or small molecule tyrosine kinase inhibitors. The only EGFR inhibitor currently approved for the treatment of NSCLC is erlotinib, a small molecule tyrosine kinase inhibitor. Although women, nonsmokers, patients with adenocarcinoma and patients with Asian ethnicity seem to have better outcomes with erlotinib, the factors predictive for response to these agents are currently the focus of investigation.
表皮生长因子是一种 170kD 的蛋白质，它与细胞表面的特定酪氨酸激酶受体，即表皮生长因子受体（EGFR）结合。EGFR 功能在包括非小细胞肺癌（NSCLC）在内的各种恶性肿瘤中失调，导致包括 K-RAS、PIK3 和 STAT3 和 STAT5 在内的几个信号转导途径的激活，促进细胞周期进程、增殖、侵袭、血管生成，并抑制细胞凋亡。EGFR 在大多数 NSCLC 病例中过度表达，但它的预后作用存在争议。目前正在 NSCLC 中进行临床试验的 EGFR 抑制剂包括单克隆抗体或小分子酪氨酸激酶抑制剂。目前唯一批准用于治疗 NSCLC 的 EGFR 抑制剂是厄洛替尼，一种小分子酪氨酸激酶抑制剂。尽管女性、不吸烟者、腺癌患者和亚洲人种似乎对厄洛替尼有更好的疗效，但目前正在研究这些药物的反应预测因素。
