Reading dynamic kinase activity in living cells for high-throughput screening.

Michael D. Allen, Lisa M. DiPilato, Meghdad Rahdar, Yunzhao R. Ren, Curtis Chong, Jun O. Liu, Jin Zhang

Research output: Contribution to journalLetterpeer-review

89 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)371-376
Number of pages6
JournalACS chemical biology
Issue number6
StatePublished - Jul 21 2006
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine


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