Pajusola K, Aprelikova O, Pelicci G, Weich H, Claesson-Welsh L, Alitalo K
Department of Pathology, University of Helsinki, Finland.
Oncogene. 1994 Dec;9(12):3545-55.
The FLT4, FLT1 and KDR/FLK1 genes encode structurally similar endothelial cell receptor tyrosine kinases. Recently it has been shown that the FLT1 and KDR/FLK-1 proteins function as high-affinity receptors for vascular endothelial growth factor (VEGF). Here we show that FLT4 does not act as a receptor for VEGF, as VEGF did not show specific binding to the FLT4 tyrosine kinase or induce its autophosphorylation. Also, FLT4 did not interact with KDR in response to VEGF. However, when fused with the ligand binding domain of the colony stimulating factor-1 receptor (CSF-1R), the FLT4 tyrosine kinase was specifically activated by CSF-1. The activated FLT4 tyrosine kinase domain was found to interact with the Src homology 2 domains of the SHC and GRB2 adaptor proteins in vitro and with SHC in cells. CSF-1 stimulation of the CSF-1R/FLT4 receptor chimera induced thymidine incorporation in serum-starved NIH3T3 fibroblasts, but not in porcine aortic or murine lung capillary endothelial cells, although tyrosyl phosphorylation of the receptor and SHC occurred in these cells as well. These results suggest that the endothelial cell FLT4 receptor tyrosine kinase transmits signals for an as yet unidentified growth factor.
FLT4、FLT1和KDR/FLK1基因编码结构相似的内皮细胞受体酪氨酸激酶。最近有研究表明,FLT1和KDR/FLK-1蛋白作为血管内皮生长因子(VEGF)的高亲和力受体发挥作用。在此我们发现,FLT4并非VEGF的受体,因为VEGF未显示出与FLT4酪氨酸激酶的特异性结合,也未诱导其自身磷酸化。此外,FLT4在VEGF作用下不与KDR相互作用。然而,当与集落刺激因子-1受体(CSF-1R)的配体结合域融合时,FLT4酪氨酸激酶可被CSF-1特异性激活。在体外,活化的FLT4酪氨酸激酶结构域可与SHC和GRB2衔接蛋白的Src同源2结构域相互作用,在细胞中则可与SHC相互作用。CSF-1对CSF-1R/FLT4受体嵌合体的刺激可诱导血清饥饿的NIH3T3成纤维细胞掺入胸苷,但在猪主动脉或鼠肺毛细血管内皮细胞中则不然,尽管这些细胞中也发生了受体和SHC的酪氨酸磷酸化。这些结果表明,内皮细胞FLT4受体酪氨酸激酶可传递来自一种尚未明确的生长因子的信号。