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Drug platforms

Fluorescent cellular assays that monitor protein tyrosine phosphatase activity

Fluorescent cellular assays that monitor tyrosine phosphatase activity could be useful for drug screening. The assay uses a human T cell line incubated with cell-permeable, phosphorylated peptides that emit a fluorescent signal when dephosphorylated by tyrosine phosphatases. The assay was used to screen chemical libraries for small molecule inhibitors of tyrosine phosphatase CD45 and identified four hits. In a validation study using human T cell and macrophage cell lines, the four hits inhibited CD45. Next steps include developing probes selective for other phosphatases.

SciBX 5(33); doi:10.1038/scibx.2012.884
Published online Aug. 23, 2012

Patent application filed covering system to monitor intracellular phosphatase activity; available for licensing from the University of Southern California
Contact: Chris Moulding, University of Southern California, Los Angeles, Calif.
e-mail:
moulding@stevens.usc.edu

Stanford, S.M. et al. Proc. Natl. Acad. Sci. USA; published online Aug. 13, 2012;
doi:10.1073/pnas.1205028109
Contact: Nunzio Bottini, La Jolla Institute for Allergy & Immunology, La Jolla, Calif.
e-mail:
nunzio@liai.org