药学学报, 2020, 55(5): 821-831
周晓菲, 李睿, 姚红娟, 李亮. ACK1小分子抑制剂的研究进展[J]. 药学学报, 2020, 55(5): 821-831.
ZHOU Xiao-fei, LI Rui, YAO Hong-juan, LI Liang. Advances in small molecule inhibitors of ACK1[J]. Acta Pharmaceutica Sinica, 2020, 55(5): 821-831.

周晓菲, 李睿, 姚红娟, 李亮
中国医学科学院、北京协和医学院医药生物技术研究所, 北京 100050
Advances in small molecule inhibitors of ACK1
ZHOU Xiao-fei, LI Rui, YAO Hong-juan, LI Liang
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
ACK1 (activated Cdc42-associated kinase) is a non-receptor tyrosine kinase, originally identified by its binding to the GTP-binding small GTPase Cdc42. It is widely expressed in human tissues and activated by various extracellular growth factors such as EGF, PDGF and TGF-β. The activated ACK1 mediates the signaling cascade by interacting with downstream effectors followed by their phosphorylation. In recent years, researchers have investigated the biological functions of ACK1 and its roles in cancer research. The gene amplification and overexpression of ACK1 is associated with a poor prognosis and metastasis in a variety of cancers including lung, ovarian and prostate cancers. Therefore, the development of small molecule inhibitors of ACK1 provides promising opportunities for cancer-targeted therapy. In this review, we briefly describe recent advances in understanding the activation and biological function of ACK1 and introduce its novel inhibitors with potential therapeutic activities in preclinical studies.
Key words:   
收稿日期: 2019-10-22
DOI: 10.16438/j.0513-4870.2019-0831
基金项目: 国家自然科学基金资助项目(81302728,81472787,81773671,81828010);CAMS医学创新基金资助项目(2016-I2M-3-013);中国药物创新重大项目(2018ZX09711001-007).
通讯作者: 李亮,Tel:86-10-83166673,E-mail:liliang@imb.pumc.edu.cn
Email: liliang@imb.pumc.edu.cn
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