Chin. J. Org. Chem. ›› 2011, Vol. 31 ›› Issue (10): 1595-1595. Previous Articles     Next Articles

Reviews

蛋白酪氨酸激酶小分子抑制剂的研究新进展

王勇,龙亚秋*   

  1. (中国科学院上海药物研究所新药研究国家重点实验室 上海 201203)
  • 收稿日期:2010-12-29 修回日期:2011-02-28 出版日期:2011-10-25 发布日期:2011-03-28
  • 通讯作者: 龙亚秋 E-mail:yqlong@mail.shcnc.ac.cn

Advances in Small-Molecule Inhibitors of Protein Tyrosine Kinases

WANG Yong, LONG Ya-Qiu   

  1. (State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sci-ences, Shanghai 201203)
  • Received:2010-12-29 Revised:2011-02-28 Online:2011-10-25 Published:2011-03-28

Protein tyrosine kinases (PTKs) play a pivotal role in the signal transduction pathways, and their deregulation is highly related with the oncology including bladder, breast, colon, and lung cancers. Com-pounds that inhibit the kinase activity of PTKs are potential chemotherapeutics to treat tumors. With the emergence of the multiple drug resistance of tumor cells against the existing PTK inhibitors, new mechanism PTK inhibitors are designed and developed. This review is focused on the recent advance of the discovery and development of the small molecular PTK inhibitors, categorized according to the mode of ac-tion. Furthermore, the synthesis of the typical structures is described.

Key words: tyrosine kinases, inhibitors, cancer, DFG motif, molecular targeted therapy