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Advances in small molecule inhibitors of ACK1
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Xiao-fei ZHOU, Rui LI, Hong-juan YAO, Liang LI*
Acta Pharmaceutica Sinica | 2020, 55(5) : 821 - 831
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Acta Pharmaceutica Sinica | 2020, 55(5): 821-831
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Advances in small molecule inhibitors of ACK1
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Xiao-fei ZHOU, Rui LI, Hong-juan YAO, Liang LI*
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  • Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2020-05-12 doi: 10.16438/j.0513-4870.2019-0831
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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.

activated Cdc42-associated kinase  /  targeted anti-cancer drug  /  non-receptor tyrosine kinase  /  small molecule inhibitor
Xiao-fei ZHOU, Rui LI, Hong-juan YAO, Liang LI. Advances in small molecule inhibitors of ACK1[J]. Acta Pharmaceutica Sinica, 2020 , 55 (5) : 821 -831 . DOI: 10.16438/j.0513-4870.2019-0831
Year 2020 volume 55 Issue 5
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Article Info
doi: 10.16438/j.0513-4870.2019-0831
  • Receive Date:2019-10-22
  • Online Date:2026-01-21
  • Published:2020-05-12
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  • Received:2019-10-22
  • Revised:2019-11-28
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    Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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