Inhibition of the Ras-dependent mitogenic pathway by phosphopeptide prodrugs with antiproliferative properties

Authors
Liu, WQ Vidal, M Mathe, C Perigaud, C Garbay, C
Citation
Wq. Liu et al., Inhibition of the Ras-dependent mitogenic pathway by phosphopeptide prodrugs with antiproliferative properties, BIOORG MED, 10(7), 2000, pp. 669-672
Citations number
32
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
7
Year of publication
2000
Pages
669 - 672
Database
ISI
SICI code
0960-894X(20000403)10:7<669:IOTRMP>2.0.ZU;2-Z
Abstract
Phosphopeptide prodrugs bearing two S-acyl-2-thioethyl (SATE) biolabile pho sphate protections were developed. They are capable to inhibit the Shc/Grb2 interaction and MAP kinases (ERK1 and ERK2) phosphorylation in cellular as say. The S-acetyl-2-thioethyl (MeSATE) analogue showed an IC50 of 1 mu M in the inhibition of the colony formation of tumor cell line NIH3T3/HER2. (C) 2000 Elsevier Science Ltd. All rights reserved.