A rapid method for generation of selective Sox-based chemosensors of Ser/Thr kinases using combinatorial peptide libraries

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1258-60. doi: 10.1016/j.bmcl.2008.12.090. Epub 2008 Dec 27.

Abstract

A novel screening method to identify selective Sox-based fluorescent probes for Ser/Thr kinases has been developed. Peptide libraries were exposed to a kinase of interest and the products of the timed reaction were analyzed by MALDI-TOF. To demonstrate the potential of this methodology, a selective substrate for Aurora A kinase was identified that showed a 7-fold improvement in catalytic efficiency over the best substrate described to date in the literature.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Aurora Kinases
  • Catalysis
  • Combinatorial Chemistry Techniques*
  • Fluorescent Dyes
  • Peptide Library
  • Protein Serine-Threonine Kinases / chemistry
  • Protein Serine-Threonine Kinases / metabolism*
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization

Substances

  • Fluorescent Dyes
  • Peptide Library
  • Aurora Kinases
  • Protein Serine-Threonine Kinases