药物发现
小分子
功能(生物学)
药物开发
计算生物学
药品
激酶
铅化合物
G蛋白偶联受体
化学
化学生物学
药理学
生物信息学
变构调节
可药性
生物
药物重新定位
蛋白激酶A
高通量筛选
制药工业
药学
受体
细胞生物学
生物化学
体外
作者
Graham L. Simpson,Jennifer Hughes,Yoshiaki Washio,Sophie Bertrand
出处
期刊:PubMed
日期:2009-09-01
卷期号:12 (5): 585-96
被引量:6
摘要
The pharmaceutical industry has traditionally targeted the inhibition of dysregulated kinases to treat diseases such as cancer and inflammatory disorders. In contrast to the human genome sequencing project, which aimed to identify novel biological targets, the possibility of activating kinases uses known targets in a novel manner. In an approach that is similar to other target classes (eg, GPCRs and nuclear receptors), transient upregulation of kinase function using small molecules has been increasingly demonstrated to lead to favorable disease outcomes. This review discusses direct small-molecule kinase activators: specifically, how these molecules were discovered, characterized, evaluated and developed into drug leads. The choice of potential targets, the mechanisms of activation and the common strategies used to discover activators are also highlighted.
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