Roof R W, Haskell M D, Dukes B D, Sherman N, Kinter M, Parsons S J
Department of Microbiology and Cancer Center, University of Virginia Health Sciences Center, Charlottesville, Virginia 22908, USA.
Mol Cell Biol. 1998 Dec;18(12):7052-63. doi: 10.1128/MCB.18.12.7052.
p190 RhoGAP is a 190-kDa protein that stably associates with p120 RasGAP and regulates actin dynamics through members of the Rho family of small GTPases. Previous studies have indicated a direct relationship between levels of p190 tyrosine phosphorylation, the extent and kinetics of epidermal growth factor (EGF)-induced actin rearrangements, and EGF-induced cell cycle progression, suggesting that p190 links Ras-mediated mitogenic signaling with signaling through the actin cytoskeleton. Determining which tyrosine residues in p190 are phosphorylated, what factors regulate phosphorylation of these sites, and what effect tyrosine phosphorylation has on p190 function is key to understanding the role(s) that p190 may play in these processes. To begin investigating these questions, we used biochemical approaches to characterize the number and relative levels of in vivo-phosphorylated tyrosine residues on endogenous p190 from C3H10T1/2 murine fibroblasts. Only two tryptic phosphopeptides containing phosphotyrosine (p-Tyr), a major site, identified as Y1105, and a minor, unidentified site, were detected. Phosphorylation of Y1105, but not the minor site, was modulated in vivo to a greater extent by overexpression of c-Src than by the EGF receptor and was efficiently catalyzed by c-Src in vitro, indicating that Y1105 is a selective and preferential target of c-Src both in vitro and in vivo. In vitro and in vivo coprecipitation analysis using glutathione S-transferase (GST) fusion proteins containing wild-type and Y1105F variants of the p190 middle domain, variants of full-length p190 ectopically expressed in COS-7 cells, and endogenous p190 and p120 in C3H10T1/2 cells revealed that p190 could bind to p120 in the presence and absence of p190 tyrosine phosphorylation. p-Tyr-independent complexes comprised 10 to 20% of the complexes formed in the presence of p-Tyr. Mutation of Y1105 from Tyr to Phe resulted in complete loss of p-Tyr-dependent complex formation, indicating that p-Y1105 was the sole p-Tyr residue mediating binding to p120. These studies describe a specific mechanism by which c-Src can regulate p190-p120 association and also document a significant role for p-Tyr-independent means of p190-p120 binding.
p190 RhoGAP是一种190 kDa的蛋白质,它与p120 RasGAP稳定结合,并通过小GTP酶Rho家族的成员调节肌动蛋白动力学。先前的研究表明,p190酪氨酸磷酸化水平、表皮生长因子(EGF)诱导的肌动蛋白重排的程度和动力学以及EGF诱导的细胞周期进程之间存在直接关系,这表明p190将Ras介导的促有丝分裂信号与通过肌动蛋白细胞骨架的信号联系起来。确定p190中哪些酪氨酸残基被磷酸化、哪些因素调节这些位点的磷酸化以及酪氨酸磷酸化对p190功能有何影响,是理解p190在这些过程中可能发挥的作用的关键。为了开始研究这些问题,我们使用生化方法来表征来自C3H10T1/2小鼠成纤维细胞的内源性p190上体内磷酸化酪氨酸残基的数量和相对水平。仅检测到两个含有磷酸酪氨酸(p-Tyr)的胰蛋白酶磷酸肽,一个主要位点,鉴定为Y1105,以及一个次要的、未鉴定的位点。与EGF受体相比,c-Src的过表达在体内对Y1105的磷酸化(而非次要位点的磷酸化)的调节程度更大,并且c-Src在体外能有效地催化Y1105的磷酸化,这表明Y1105在体外和体内都是c-Src的选择性和优先靶点。使用含有p190中间结构域的野生型和Y1105F变体的谷胱甘肽S-转移酶(GST)融合蛋白、在COS-7细胞中异位表达的全长p190变体以及C3H10T1/2细胞中的内源性p190和p120进行的体外和体内共沉淀分析表明,在存在和不存在p190酪氨酸磷酸化的情况下,p190都能与p120结合。不依赖p-Tyr的复合物占在存在p-Tyr的情况下形成的复合物的10%至20%。将Y1105从酪氨酸突变为苯丙氨酸导致完全丧失依赖p-Tyr的复合物形成,这表明p-Y1105是介导与p120结合的唯一p-Tyr残基。这些研究描述了一种c-Src可以调节p190-p120结合的特定机制,并且还证明了不依赖p-Tyr的p190-p120结合方式的重要作用。