Stein D, Wu J, Fuqua S A, Roonprapunt C, Yajnik V, D'Eustachio P, Moskow J J, Buchberg A M, Osborne C K, Margolis B
New York University Medical Center, Department of Pharmacology, Kaplan Cancer Center, NY 10016.
EMBO J. 1994 Mar 15;13(6):1331-40. doi: 10.1002/j.1460-2075.1994.tb06386.x.
SH2 domain proteins are important components of the signal transduction pathways activated by growth factor receptor tyrosine kinases. We have been cloning SH2 domain proteins by bacterial expression cloning using the tyrosine phosphorylated C-terminus of the epidermal growth factor receptor as a probe. One of these newly cloned SH2 domain proteins, GRB-7, was mapped on mouse chromosome 11 to a region which also contains the tyrosine kinase receptor, HER2/erbB-2. The analogous chromosomal locus in man is often amplified in human breast cancer leading to overexpression of HER2. We find that GRB-7 is amplified in concert with HER2 in several breast cancer cell lines and that GRB-7 is overexpressed in both cell lines and breast tumors. GRB-7, through its SH2 domain, binds tightly to HER2 such that a large fraction of the tyrosine phosphorylated HER2 in SKBR-3 cells is bound to GRB-7. GRB-7 can also bind tyrosine phosphorylated SHC, albeit at a lower affinity than GRB2 binds SHC. We also find that GRB-7 has a strong similarity over > 300 amino acids to a newly identified gene in Caenorhabditis elegans. This region of similarity, which lies outside the SH2 domain, also contains a pleckstrin homology domain. The presence of evolutionarily conserved domains indicates that GRB-7 is likely to perform a basic signaling function. The fact that GRB-7 and HER2 are both overexpressed and bound tightly together suggests that this basic signaling pathway is greatly amplified in certain breast cancers.
SH2结构域蛋白是由生长因子受体酪氨酸激酶激活的信号转导通路的重要组成部分。我们一直使用表皮生长因子受体的酪氨酸磷酸化C末端作为探针,通过细菌表达克隆来克隆SH2结构域蛋白。这些新克隆的SH2结构域蛋白之一GRB-7,被定位在小鼠11号染色体上的一个区域,该区域也包含酪氨酸激酶受体HER2/erbB-2。人类中类似的染色体位点在乳腺癌中常被扩增,导致HER2过表达。我们发现,在几种乳腺癌细胞系中,GRB-7与HER2协同扩增,并且GRB-7在细胞系和乳腺肿瘤中均过表达。GRB-7通过其SH2结构域与HER2紧密结合,使得SKBR-3细胞中大部分酪氨酸磷酸化的HER2与GRB-7结合。GRB-7也能结合酪氨酸磷酸化的SHC,尽管其亲和力低于GRB2与SHC的结合。我们还发现,GRB-7在超过300个氨基酸的区域与秀丽隐杆线虫中一个新鉴定的基因有很强的相似性。这个相似区域位于SH2结构域之外,也包含一个普列克底物蛋白同源结构域。进化保守结构域的存在表明GRB-7可能执行一种基本的信号功能。GRB-7和HER2均过表达且紧密结合在一起,这一事实表明在某些乳腺癌中,这条基本的信号通路被极大地放大了。