Deanna G Adams, Yu Wang, Puiying A Mak, Jason Chyba, Orzala Shalizi, Jason Matzen, Paul Anderson, Tim R Smith, Michael Garcia, Genevieve L Welch, Emmanuel J Claret, Michel Fink, Anthony P Orth, Jeremy S Caldwell, Achim Brinker
High-throughput cellular profiling has successfully stimulated early drug discovery pipelines by facilitating targeted as well as opportunistic lead finding, hit annotation and SAR analysis. While automation-friendly universal assay formats exist to address most established drug target classes like GPCRs, NHRs, ion channels or Tyr-kinases, no such cellular assay technology is currently enabling an equally broad and rapid interrogation of the Ser/Thr-kinase space. Here we present the foundation of an emerging cellular Ser/Thr-kinase platform that involves a) coexpression of targeted kinases with promiscuous peptide substrates and b) quantification of intracellular substrate phosphorylation by homogeneous TR-FRET...
May 23, 2008: Current Chemical Genomics