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Inhibition of the ras-dependent mitogenic pathway by phosphopeptide prodrugs with antiproliferative properties
1Laboratoire de Pharmacochimie Moléculaire et Structurale, U266 INSERM, UMR 8600 CNRS, Faculté de Pharmacie, Paris, France.
Bioorganic & Medicinal Chemistry Letters
|April 13, 2000
Abstract:
Phosphopeptide prodrugs bearing two S-acyl-2-thioethyl (SATE) biolabile phosphate protections were developed. They are capable to inhibit the Shc/Grb2 interaction and MAP kinases (ERK1 and ERK2) phosphorylation in cellular assay. The S-acetyl-2-thioethyl (MeSATE) analogue showed an IC50 of 1 microM in the inhibition of the colony formation of tumor cell line NIH3T3/HER2.