School of Medicine, Xi'an Jiaotong University, No. 76, Yanta West Road, 710061, Xi'an, ShaanXi Province, P.R. China.
Curr Med Chem. 2014;21(11):1336-50. doi: 10.2174/0929867320666131119124646.
Dysregulation of receptor tyrosine kinases (RTKs) in cancer cells is extremely common. Overexpression of human epidermal growth factor receptor (EGFR/HER) tyrosine kinase is correlated with tumor aetiology, progression and poor prognosis. Their activation is also observed frequently in human cancers. Therefore, RTKs have been identified as important therapeutic targets in oncology. Many therapeutic methods have been developed based on inhibition of EGFR and HER-2. Herein, we will discuss recent progress in the development of EGFR/HER-2 tyrosine kinase inhibitors. We will focus on the design strategies, pharmacological profiles and structure-activity relationships (SARs) of EGFR and HER-2 inhibitors.
癌细胞中受体酪氨酸激酶 (RTKs) 的失调极为常见。人表皮生长因子受体 (EGFR/HER) 酪氨酸激酶的过度表达与肿瘤病因、进展和预后不良相关。在人类癌症中也经常观察到它们的激活。因此，RTKs 已被确定为肿瘤学中重要的治疗靶点。许多治疗方法都是基于抑制 EGFR 和 HER-2 而开发的。本文将讨论 EGFR/HER-2 酪氨酸激酶抑制剂研发的最新进展。我们将重点介绍 EGFR 和 HER-2 抑制剂的设计策略、药理学特征和构效关系 (SAR)。
