Soler C, Alvarez C V, Beguinot L, Carpenter G
Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-0146.
Oncogene. 1994 Aug;9(8):2207-15.
The importance of epidermal growth factor (EGF) receptor expression level and autophosphorylation sites in src homology and collagen protein (SHC) tyrosine phosphorylation has been studied. In contrast to EGF-induced tyrosine phosphorylation of the GTPase-activating protein for ras (rasGAP) and phospholipase C-gamma 1 (PLC-gamma 1), SHC tyrosine phosphorylation occurs at a very low receptor density in parental NIH3T3 mouse fibroblasts expressing less than 1 x 10(4) EGF receptors per cell. In transfected NIH3T3 cells expressing human EGF receptors (approximately 4 x 10(5) receptors per cell), maximal levels of SHC and PLC-gamma 1 tyrosine phosphorylation occur when approximately 4 x 10(4) receptors or more are occupied by ligand. At lower levels of receptor occupancy only SHC phosphorylation was significant. Also, EGF treatment of mouse keratinocytes, which represent a physiological target of EGF, express a low number of EGF receptors (approximately 2 x 10(4) receptors per cell), and stringently require EGF to grow, results in intense SHC tyrosine phosphorylation, compared to rasGAP or PLC-gamma 1. SHC is also efficiently tyrosine phosphorylated by an EGF receptor deletion mutant (Dc214) that is devoid of autophosphorylation sites, but which remains mitogenically responsive to EGF. The EGF receptor mutant Dc214 is able to activate the ras guanine nucleotide exchanger and phosphorylate mitogen-activated protein kinase (MAPK), presumable as a result of complex formation between tyrosine phosphorylated SHC and GRB2. These results indicate that potent EGF-induced SHC tyrosine phosphorylation can be triggered in cells having relatively few receptors. Also, our data show that EGF receptors are able to phosphorylate SHC, activate the exchange of guanine nucleotide on ras and phosphorylate MAPK by a mechanism that does not require receptor autophosphorylation sites and, therefore, the src homology 2 (SH2):phosphotyrosine-dependent interaction of SHC or GRB2 with the EGF receptor.
表皮生长因子(EGF)受体表达水平以及src同源和胶原蛋白(SHC)酪氨酸磷酸化中的自磷酸化位点的重要性已得到研究。与EGF诱导的ras的GTP酶激活蛋白(rasGAP)和磷脂酶C-γ1(PLC-γ1)的酪氨酸磷酸化相反,在每个细胞表达少于1×10⁴个EGF受体的亲本NIH3T3小鼠成纤维细胞中,SHC酪氨酸磷酸化在非常低的受体密度下发生。在表达人EGF受体(每个细胞约4×10⁵个受体)的转染NIH3T3细胞中,当约4×10⁴个或更多受体被配体占据时,SHC和PLC-γ1酪氨酸磷酸化达到最大水平。在较低的受体占据水平下,只有SHC磷酸化是显著的。此外,EGF处理小鼠角质形成细胞,其代表EGF的生理靶标,表达少量的EGF受体(每个细胞约2×10⁴个受体),并且严格需要EGF来生长,与rasGAP或PLC-γ1相比,会导致强烈的SHC酪氨酸磷酸化。SHC也能被一个缺乏自磷酸化位点但对EGF仍有促有丝分裂反应的EGF受体缺失突变体(Dc214)有效地酪氨酸磷酸化。EGF受体突变体Dc214能够激活ras鸟嘌呤核苷酸交换因子并磷酸化丝裂原活化蛋白激酶(MAPK),推测这是酪氨酸磷酸化的SHC和GRB2之间形成复合物的结果。这些结果表明,在受体相对较少的细胞中也能触发强效的EGF诱导的SHC酪氨酸磷酸化。此外,我们的数据表明,EGF受体能够磷酸化SHC,激活ras上的鸟嘌呤核苷酸交换,并通过一种不需要受体自磷酸化位点的机制磷酸化MAPK,因此,也不需要SHC或GRB2与EGF受体的src同源2(SH2):磷酸酪氨酸依赖性相互作用。