Craddock B L, Hobbs J, Edmead C E, Welham M J
Department of Pharmacy and Pharmacology, the University of Bath, Bath BA2 7AY, United Kingdom.
J Biol Chem. 2001 Jun 29;276(26):24274-83. doi: 10.1074/jbc.M009098200. Epub 2001 May 2.
We have demonstrated previously that class I(A) phosphoinositide 3-kinases play a major role in regulation of interleukin-3 (IL)-3-dependent proliferation. Investigations into the downstream targets involved have identified the MAPK cascade as a target. Expression of Deltap85 and incubation with LY294002 both inhibited IL-3-induced activation of Mek, Erk1, and Erk2. This was most pronounced during the initial phase of Erk activation. The Mek inhibitor, PD98059, blocked IL-3-driven proliferation, an effect enhanced by Deltap85 expression, suggesting that inhibition of Mek and Erks by Deltap85 contributes to the decrease in IL-3-induced proliferation in these cells but that additional pathways may also be involved. To investigate the mechanism leading to decreased activation of Erks, we investigated effects on SHP2 and Gab2, both implicated in IL-3 regulation of Erk activation. Expression of Deltap85 led to a reduction in SHP2 tyrosine phosphorylation and its ability to interact with Grb2 and Gab2 but increased overall tyrosine phosphorylation of Gab2. LY294002 did not perturb SHP2 interactions, potentially related to differences in the effects of these inhibitors on levels of phosphoinositides. These results imply that the regulation of Erks by class I(A) phosphoinositide 3-kinase may contribute to IL-3-driven proliferation and that both SHP2 and Gab2 are possibly involved in this regulation.
我们之前已经证明,I(A)类磷酸肌醇3激酶在白细胞介素-3(IL-3)依赖性增殖的调节中起主要作用。对所涉及的下游靶点的研究已确定丝裂原活化蛋白激酶(MAPK)级联反应是一个靶点。Delta p85的表达以及与LY294002共同孵育均抑制了IL-3诱导的Mek、Erk1和Erk2的活化。这在Erk活化的初始阶段最为明显。Mek抑制剂PD98059阻断了IL-3驱动的增殖,Delta p85表达增强了这种作用,这表明Delta p85对Mek和Erks的抑制作用导致了这些细胞中IL-3诱导的增殖减少,但可能还涉及其他途径。为了研究导致Erks活化减少的机制,我们研究了对SHP2和Gab2的影响,它们都与IL-3对Erk活化的调节有关。Delta p85的表达导致SHP2酪氨酸磷酸化及其与Grb2和Gab2相互作用的能力降低,但Gab2的总体酪氨酸磷酸化增加。LY294002并未干扰SHP2的相互作用,这可能与这些抑制剂对磷酸肌醇水平影响的差异有关。这些结果表明,I(A)类磷酸肌醇3激酶对Erks的调节可能有助于IL-3驱动的增殖,并且SHP2和Gab2可能都参与了这种调节。