Progress with covalent small-molecule kinase inhibitors

被引：142
|
作者：
Zhao, Zheng [1 ]
Bourne, Philip E. [1 ]
机构：
[1] Univ Virginia, Dept Biomed Engn, Charlottesville, VA 22908 USA
来源：
DRUG DISCOVERY TODAY | 2018年 / 23卷 / 03期
关键词：
CELL LUNG-CANCER; ATP-BINDING SITE; IRREVERSIBLE INHIBITORS; PROTEIN-KINASES; DRUG DISCOVERY; TYROSINE KINASE; TREATMENT STRATEGIES; EGFR INHIBITORS; HUMAN KINOME; RESISTANCE;
D O I：
10.1016/j.drudis.2018.01.035
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
With reduced risk of toxicity and high selectivity, covalent small-molecule kinase inhibitors (CSKIs) have emerged rapidly. Through the lens of structural system pharmacology, here we review this rapid progress by considering design strategies and the challenges and opportunities offered by current CSKIs.
引用
收藏
页码：727 / 735
页数：9
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