血小板衍生生长因子受体PDGFR抑制剂的研究进展.pdfVIP

- 2 - 肿瘤药学 2013 年 2 月第 3 卷第 1 期　Anti-tumor Pharmacy, February 2013, Vol. 3, No. 1 ●综　　述● 血小板衍生生长因子受体 （PDGFR）抑制剂 的研究进展★ 李代洪，艾俊涛，谢　欣，胡高云，李乾斌* （中南大学药学院，湖南　长沙， 100 13 ） 摘要：血小板衍生生长因子（platelet-derived growth factor, PDGF）是一种重要的促有丝分裂因子，与多种疾病的 发生有关，PDGF 发挥其生理作用是通过血小板衍生生长因子受体（platelet-derived growth factor receptor, PDGFR） 介导的细胞信号传导实现的，PDGFR 是一种酪氨酸蛋白激酶受体，已成为肿瘤等多种疾病的治疗靶点。目前已开 发了喹喔啉、喹唑啉、吲哚酮等多种结构的 PDGFR 抑制剂，并有伊马替尼、苏尼替尼等多种抑制剂上市或进入临 床实验研究阶段。本文旨在对 PDGF 的结构与功能以及 PDGFR 抑制剂的研究进展进行综述。 关键词：血小板衍生生长因子；血小板衍生生长因子受体；小分子抑制剂；肿瘤 中图分类号：R730.23　文献标识码 ：A　文章编号：2095-1264（2013）01-0002-06 doi：10.3969/j.issn.2095-1264.2013.001 Research Progress on Platelet-derived Growth Factor Receptor Inhibitors Li Daihong, Ai Juntao, Xie Xin, Hu Gaoyun, Li Qianbin* (Dep artment of Medicinal Chemistry, School of Pharmaceutical Sciences, Central South University, Changsha, Hu- nan, 410013, China) Abstract: Platelet-derived growth factor (PDGF) is a significant mitogen, which has been proved to be related to many diseases. PDGF physiological function works through the signal transduction mediated by platelet-derived growth factor re- ceptor (PDGFR). PDGFR, a tyrosine kinase receptor, has become therapy targets of many diseases, such as cancer. So far many PDGFR inhibitors have been developed of various chemical structures such as quinoxaline, quinazoline and indolone. Several inhibitors like imatinib and sunitinib have come to market or gotten into clinical trials. This article is aimed to introduce the structure and function of PDGF as well as the research progress on platelet-derived growth fac