药学学报, 2021, 56(2): 414-431
龙春庭, 邵敏, 陆小云. 激酶小分子抑制剂研究进展[J]. 药学学报, 2021, 56(2): 414-431.
LONG Chun-ting, SHAO Min, LU Xiao-yun. Research progress on small molecule kinase inhibitors[J]. Acta Pharmaceutica Sinica, 2021, 56(2): 414-431.

龙春庭, 邵敏, 陆小云
暨南大学药学院, 广东 广州 510632
关键词:    蛋白激酶      小分子抑制剂      抗肿瘤      批准上市     
Research progress on small molecule kinase inhibitors
LONG Chun-ting, SHAO Min, LU Xiao-yun
College of Pharmacy, Jinan University, Guangzhou 510632, China
Protein kinases are intimately involved in the pathogenesis of many diseases such as cancer, inflammation, and autoimmune and neurological diseases. Therefore, kinases have been widely studied as drug targets over the past three decades. As of April, 2020, the FDA had approved 59 small molecule kinase inhibitors (SMKIs) in the emerging field of targeted drug therapy. This paper focuses on the biochemistry and pharmacology of these 59 SMKIs and 121 SMKIs for which structures can be retrieved and that are now in phase Ⅱ and Ⅲ clinical trials. In addition, this paper also conducts a simple analysis of several popular targets and their inhibitors.
Key words:    protein kinase    small molecule kinase inhibitor    anticancer    approved   
收稿日期: 2020-06-20
DOI: 10.16438/j.0513-4870.2020-1027
基金项目: 国家自然科学基金资助项目(81922062,81874285).
通讯作者: 陆小云,E-mail:luxy2016@jnu.edu.cn
Email: luxy2016@jnu.edu.cn
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