Homma Y, Homma M
Dept. of Biomolecular Sciences, Fukushima Medical College.
Gan To Kagaku Ryoho. 1997 Sep;24(11):1611-7.
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.
N-肉豆蔻酰化PCI肽（myr-PCI）最初是基于PLC-γ2的PCI序列开发的，它在体外可抑制纯化的PLC同工型的活性以及瑞士3T3细胞中依赖外部刺激的IP3形成。当将myr-PCI添加到源自家族性腺瘤性息肉病患者的KMS-8细胞中时，它也抑制了血清依赖性IP3形成、DNA合成和细胞生长。为了开发具有强抗PLC活性的PCI肽，我们合成了N端和/或C端被多种化合物酰化的肽，并检测了它们的抗PLC和抗增殖活性。这些结果对于确定体内抑制PLC所需的最小结构将非常有帮助。
