Development and optimization of high-throughput in vitro protein phosphatase screening assays

Nat Protoc. 2007;2(5):1134-44. doi: 10.1038/nprot.2007.155.

Abstract

We describe here detailed protocols to design, optimize and validate in vitro phosphatase assays that we have utilized to conduct high-throughput screens for inhibitors of dual-specificity phosphatases: CDC25B, mitogen-activated protein kinase phosphatase (MKP)-1 and MKP-3. We provide details of the critical steps that are needed to effectively miniaturize the assay into a 384-well, high-throughput format that is both reproducible and cost effective. In vitro phosphatase assays that are optimized according to these protocols should satisfy the assay performance criteria required for a robust high-throughput assay with Z-factors >0.5, and with low intra-plate, inter-plate and day-to-day variability (CV <20%). Assuming the availability of sufficient active phosphatase enzyme and access to appropriate liquid handling automation and detection instruments, a single investigator should be able to develop a 384-well format high-throughput assay in a period of 3-4 weeks.

MeSH terms

  • Molecular Probe Techniques*
  • Phosphoprotein Phosphatases / antagonists & inhibitors*
  • Protein Array Analysis / methods*
  • Reproducibility of Results
  • Small Molecule Libraries / isolation & purification*
  • Small Molecule Libraries / pharmacology

Substances

  • Small Molecule Libraries
  • Phosphoprotein Phosphatases