摘要
表皮生长因子受体(EGFR)属于蛋白酪氨酸激酶受体超家族一员,在肿瘤细胞生长、凋亡、侵袭和转移中具有重要作用。靶向EGFR酪氨酸激酶抑制剂已经成为抗肿瘤药物研究的热点和趋势。目前靶向EGFR酪氨酸激酶小分子抑制剂研究有了长足进展,开发出一系列具有临床应用价值的药物分子,但是大多数病人在治疗后期会因为受体氨基酸的激活突变而导致耐药性。因此对于适用于后期治疗或者可以满足长期治疗效果的药物依然是临床急需。笔者通过查阅近20年来国内、外有关文献,详细介绍靶向小分子EGFR酪氨酸激酶抑制剂的研究进展和抗肿瘤机制,为更加深入研究提供参考依据。
Epidermal growth factor receptor (EGFR), a member of the super family of protein tyrosine kinase receptors, plays a crucial role in proliferation, apoptosis, aggression and metastasis of tumor cells. The target-EGFR inhibitors have been a hotspot and tendency in the progress of anti-tumors. Currently, the target-EGFR inhibitors have made a steady progress and many valuable drugs in the clinical treatment have been developed. However, many patients will be resistance to the drugs due to the mutation of amino acid. Therefore, drugs which can be effective in the later treatment or long-term therapies will always be deficient. In this article, the research progress and mechanism of anti-tumor of small molecules EGFR inhibitors in detail are reviewed.
作者
耿传荣
邓玉晓
崔新强
赵思太
冯光玲
孙晋瑞
段崇刚
GENG Chuan-rong, DENG Yu-xiao, CUI Xin-qiang, ZHAO Si-tai, FENG Guang-ling, SUN Jin-rui, DUAN Chong-gang(Institute of Chemical Drugs, Shandong Academy of Pharmaceutical Sciences, Jinan 250101, Chin)
出处
《中国药学杂志》
CAS
CSCD
北大核心
2018年第13期1037-1046,共10页
Chinese Pharmaceutical Journal