期刊
ACS CHEMICAL BIOLOGY
卷 1, 期 6, 页码 371-376出版社
AMER CHEMICAL SOC
DOI: 10.1021/cb600202f
关键词
-
资金
- NIDDK NIH HHS [R01 DK073368] Funding Source: Medline
- NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES [R01DK073368] Funding Source: NIH RePORTER
Protein kinases, as crucial signaling molecules, represent an emerging class of drug targets, and the ability to assay their activities in living cells with high-throughput screening should provide exciting opportunities for drug discovery and chemical and functional genomics. Here, we describe a general method for high-throughput reading of dynamic kinase activities using ratiometric fluorescent sensors, and showcase an example of reading intracellular activities of protein kinase A ( PKA) and the cyclic adenosine monophosphate ( cAMP)/ PKA pathway downstream of many G-protein coupled receptors ( GPCRs). We further demonstrate the first compound screen based on the ability of compounds to modulate dynamic kinase activities in living cells and show that such screening of a collection of clinical compounds has successfully identified modulators of the GPCR/ cAMP/ PKA pathway.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据