Marra F, Pinzani M, DeFranco R, Laffi G, Gentilini P
Istituto di Medicina Interna, Università di Firenze, Italy.
FEBS Lett. 1995 Dec 4;376(3):141-5. doi: 10.1016/0014-5793(95)01261-0.
Phosphatidylinositol 3-kinase (PI 3-K) is a lipid and protein kinase which associates with the activated platelet-derived growth factor (PDGF) receptor and other tyrosine kinases. We studied the effects of wortmannin, a selective inhibitor of PI 3-K, on the activation of extracellular-signal regulated kinase (ERK) by PDGF in cultured hepatic stellate cells, mesenchymal cells responsible for extracellular matrix synthesis within the liver. Incubation with 100 nM wortmannin, a dose which almost completely blocks PI 3-K, resulted in 50% reduction of ERK activity. Direct inhibition of ERK by wortmannin could not be considered responsible for this effect, since wortmannin did not inhibit ERK activity in vitro. Rather, inhibition of PI 3-K acts on the kinase cascade that leads to ERK activation, since PDGF-dependent phosphorylation of ERK was found to be reduced after incubation with wortmannin. Wortmannin also inhibited the increase in c-fos mRNA induced by PDGF, which is dependent on ERK activation. The results of this study show that in hepatic stellate cells PI 3-K is involved in ERK activation, although it is not necessary. These data indicate cross-talk between PI 3-K and the Ras/ERK pathway in PDGF-stimulated cells.
磷脂酰肌醇3激酶(PI 3-K)是一种脂质和蛋白激酶,它与活化的血小板衍生生长因子(PDGF)受体及其他酪氨酸激酶相关联。我们研究了PI 3-K的选择性抑制剂渥曼青霉素对培养的肝星状细胞(肝脏内负责细胞外基质合成的间充质细胞)中PDGF激活细胞外信号调节激酶(ERK)的影响。用100 nM渥曼青霉素孵育(该剂量几乎可完全阻断PI 3-K)导致ERK活性降低50%。渥曼青霉素对ERK的直接抑制作用不能被认为是造成这种效应的原因,因为渥曼青霉素在体外不抑制ERK活性。相反,PI 3-K的抑制作用作用于导致ERK激活的激酶级联反应,因为在与渥曼青霉素孵育后发现PDGF依赖的ERK磷酸化减少。渥曼青霉素还抑制了PDGF诱导的c-fos mRNA增加,而这依赖于ERK激活。本研究结果表明,在肝星状细胞中PI 3-K参与了ERK激活,尽管并非必需。这些数据表明在PDGF刺激的细胞中PI 3-K与Ras/ERK途径之间存在相互作用。