摘要
表皮生长因子受体(EGFR)家族包括四个结构相关的受体酪氨酸激酶,分别为HER1 (EGFR, erbB1)、 HER2 (erbB2)、 HER3 (erbB3)和 HER4 (erbB4)。过度的HER表达信号为抗癌介入提供了一次特殊机会,在一些实体肿瘤发展中有紧密的作用。随着以EGFR家族为靶点潜在抗癌治疗的大量的药理学研究的开展,该家族的激酶抑制剂持续上升不断被开发,且进入临床研究阶段。EGFR家族小分子酪氨酸激酶抑制剂已经被批准或者进入临床研究,。在此,我们主要对其作用机制、结构-活性关系、结合模式、合成途径和临床状态进行了综述。
关键词: 临床试验,EGFR/HER/erbB, 小分子抑制剂,实体肿瘤
Current Medicinal Chemistry
Title:Development of EGFR Family Small Molecule Inhibitors for Anticancer Intervention: An Overview of Approved Drugs and Clinical Candidates
Volume: 21 Issue: 38
Author(s): Weiyan Cheng, Yongzhou Hu and Rong Sheng
Affiliation:
关键词: 临床试验,EGFR/HER/erbB, 小分子抑制剂,实体肿瘤
摘要: The epidermal growth factor receptor (EGFR) family includes four structurally related receptor tyrosine kinases, termed as HER1 (EGFR, erbB1), HER2 (erbB2), HER3 (erbB3), and HER4 (erbB4). Given its intimate role in the development of several solid tumors, excessive HER signaling provides a unique opportunity for anticancer intervention. Along with extensive pharmacological studies validating the therapeutic potential of targeting the EGFR family for cancer therapy, kinase inhibitors of this family are continuously coming up and entering clinical studies. Herein, we review the EGFR family small molecule kinase inhibitors which have been approved or progressed into clinical studies, mainly focusing on their mechanisms of action, structure-activity relationships, binding modes, synthetic routes, and clinical status.
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Cite this article as:
Cheng Weiyan, Hu Yongzhou and Sheng Rong, Development of EGFR Family Small Molecule Inhibitors for Anticancer Intervention: An Overview of Approved Drugs and Clinical Candidates, Current Medicinal Chemistry 2014; 21 (38) . https://dx.doi.org/10.2174/0929867321666140915142809
DOI https://dx.doi.org/10.2174/0929867321666140915142809 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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