Koval A P, Blakesley V A, Roberts C T, Zick Y, Leroith D
Diabetes Branch, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD 20892-1770, USA.
Biochem J. 1998 Mar 1;330 ( Pt 2)(Pt 2):923-32. doi: 10.1042/bj3300923.
The Crk proto-oncogene product is an SH2 and SH3 domain-containing adaptor protein. We have previously demonstrated that Crk-II becomes rapidly tyrosine-phosphorylated in response to stimulation with insulin-like growth factor I (IGF-I) and might be involved in the IGF-I receptor signalling pathway. To determine whether this involvement includes the direct interaction of Crk-II with the cytoplasmic region of the receptor, studies were performed in vitro with glutathione S-transferase (GST) fusion proteins containing various domains of Crk-II. The kinase assay in vitro showed that activated IGF-I receptors efficiently phosphorylated the GST-Crk-II fusion protein. This phosphorylation was dependent on the presence of the SH2 domain and Tyr-221 located in the spacer region between the two SH3 domains. Mutation of Tyr-221 not only prevented phosphorylation of GST-Crk in vitro, but also significantly increased the ability of GST-Crk proteins to co-precipitate activated IGF-I receptors from total cell lysates. Additional binding experiments in vitro showed that Crk-II might interact with the phosphorylated IGF-I receptor through its SH2 domain. To elucidate which region of the IGF-I receptor interacts with Crk-II, a peptide association assay was used in vitro. Different domains of the IGF-I receptor were expressed as (His)6-tagged fusion peptides, phosphorylated with activated wheat germ agglutinin-purified IGF-I receptors and tested for association with GST-Crk-II fusion proteins. Using wild-type as well as mutated peptides, we showed that the SH2 domain of Crk-II preferentially binds the peptide encoding the juxtamembrane region of the IGF-I receptor. Phosphorylation of Tyr-950 and Tyr-943 of the receptor is important for this interaction. These findings allow us to propose a model of direct interaction of Crk-II and the IGF-I receptor in vivo. On activation of the IGF-I receptor, Crk-II binds to phosphorylated tyrosine residues, especially in the juxtamembrane region. As a result of this binding, the IGF-I receptor kinase phosphorylates Tyr-221 of Crk-II, resulting in a change in intramolecular folding and binding of the SH2 domain to the phosphorylated Tyr-221, which causes rapid disassociation of the Crk-II-IGF-I receptor complex.
Crk原癌基因产物是一种含有SH2和SH3结构域的衔接蛋白。我们之前已经证明,Crk-II在胰岛素样生长因子I(IGF-I)刺激下会迅速发生酪氨酸磷酸化,可能参与IGF-I受体信号通路。为了确定这种参与是否包括Crk-II与受体胞质区域的直接相互作用,我们使用含有Crk-II不同结构域的谷胱甘肽S-转移酶(GST)融合蛋白进行了体外研究。体外激酶分析表明,活化的IGF-I受体能有效地使GST-Crk-II融合蛋白磷酸化。这种磷酸化依赖于SH2结构域和位于两个SH3结构域之间间隔区的Tyr-221的存在。Tyr-221的突变不仅阻止了体外GST-Crk的磷酸化,还显著增加了GST-Crk蛋白从总细胞裂解物中共沉淀活化的IGF-I受体的能力。额外的体外结合实验表明,Crk-II可能通过其SH2结构域与磷酸化的IGF-I受体相互作用。为了阐明IGF-I受体的哪个区域与Crk-II相互作用,我们在体外使用了肽结合分析。IGF-I受体的不同结构域被表达为(His)6标记的融合肽,用活化的麦胚凝集素纯化的IGF-I受体进行磷酸化,并测试与GST-Crk-II融合蛋白的结合。使用野生型以及突变肽,我们表明Crk-II的SH2结构域优先结合编码IGF-I受体近膜区域的肽。受体的Tyr-950和Tyr-943的磷酸化对于这种相互作用很重要。这些发现使我们能够提出一个Crk-II与IGF-I受体在体内直接相互作用的模型。在IGF-I受体激活时,Crk-II与磷酸化的酪氨酸残基结合,特别是在近膜区域。这种结合的结果是,IGF-I受体激酶使Crk-II的Tyr-221磷酸化,导致分子内折叠发生变化,SH2结构域与磷酸化的Tyr-221结合,从而导致Crk-II-IGF-I受体复合物迅速解离。