
N-Myristoylated PCI peptide, myr-PCI, originally developed based on the PCI sequence of PLC- gamma 2, inhibited activity of purified PLC isoforms in vitro, and external stimuli-dependent IP3 formation in Swiss 3T3 cells. When myr-PCI was added to KMS-8 cells, derived from familial adenomatous polyposis patients, it also suppressed the serum-dependent IP3 formation, DNA synthesis, and cell growth. In order to develop PCI peptides with strong anti-PLC activity, we synthesized the peptides whose N- and/or C-termini were acylated by a variety of compounds, and examined their anti-PLC and anti-proliferative activities. Results would be quite helpful to determine the minimal structure required for PLC inhibition in vivo.
3T3 Cells, Adenocarcinoma, Second Messenger Systems, Mice, Type C Phospholipases, Colonic Neoplasms, Tumor Cells, Cultured, Animals, Humans, Enzyme Inhibitors, Cell Division
3T3 Cells, Adenocarcinoma, Second Messenger Systems, Mice, Type C Phospholipases, Colonic Neoplasms, Tumor Cells, Cultured, Animals, Humans, Enzyme Inhibitors, Cell Division
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