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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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3T3 Cells
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Adaptor Proteins, Signal Transducing*
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Animals
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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GRB2 Adaptor Protein
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Intramolecular Transferases / metabolism
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Mice
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Mitogen-Activated Protein Kinase 1 / metabolism
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Mitogen-Activated Protein Kinase 3
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Mitogen-Activated Protein Kinases / metabolism
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Phosphopeptides / chemistry
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Phosphopeptides / pharmacology*
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Phosphorylation / drug effects
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Prodrugs / chemistry
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Prodrugs / pharmacology*
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Proteins / metabolism
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Stem Cells / drug effects
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ras Proteins / antagonists & inhibitors
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ras Proteins / pharmacology
Substances
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Adaptor Proteins, Signal Transducing
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Antineoplastic Agents
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GRB2 Adaptor Protein
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Grb2 protein, mouse
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Phosphopeptides
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Prodrugs
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Proteins
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Mitogen-Activated Protein Kinase 1
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Mitogen-Activated Protein Kinase 3
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Mitogen-Activated Protein Kinases
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ras Proteins
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Intramolecular Transferases
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squalene-hopene cyclase