Fluorescent monitoring of kinase activity in real time: development of a robust fluorescence-based assay for Abl tyrosine kinase activity

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3091-4. doi: 10.1016/s0960-894x(01)00650-3.

Abstract

Fluorescent biosensors hold great promise for drug discovery. Using a solid-phase version of protein semi-synthesis, we incorporated two fluorophores at specific sites within a truncated version of the c-Crk-II protein. The resulting fluorescent protein biosensor permits the real-time monitoring of Abl kinase activity and provides a robust and rapid method for assaying Abl kinase inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Biosensing Techniques
  • Enzyme Inhibitors / pharmacology
  • Proto-Oncogene Proteins c-abl / antagonists & inhibitors
  • Proto-Oncogene Proteins c-abl / metabolism*
  • Spectrometry, Fluorescence

Substances

  • Enzyme Inhibitors
  • Proto-Oncogene Proteins c-abl