Feller Stephan M, Wecklein Heike, Lewitzky Marc, Kibler Eike, Raabe Thomas
Cancer Research UK, Weatherall Institute of Molecular Medicine, John Radcliffe Hospital, Headington, Oxford OX3 9DS, UK.
Mech Dev. 2002 Aug;116(1-2):129-39. doi: 10.1016/s0925-4773(02)00147-8.
Activation of the Sevenless (Sev) receptor tyrosine kinase (RTK) in the developing Drosophila eye is required for the specification of the R7 photoreceptor cell fate. Daughter of Sevenless (Dos), a putative multi-site adaptor protein, is a substrate of the Sev kinase and is known to associate with the tyrosine phosphatase Corkscrew (Csw). Binding of Csw to Dos depends on the Csw Src homology 2 (SH2) domains and is an essential step for signaling by the Sev RTK. Dos, however, lacks a recognizable phosphotyrosine interaction domain and it was previously unclear how it is recruited to the Sev receptor. Here it is shown that the SH2/SH3 domain adaptor protein Drk can provide this link. Drk binds with its SH2 domain to the autophosphorylated Sev receptor while the C-terminal SH3 domain is able to associate with Dos. The Drk SH3 domain binding motifs on Dos were mapped to two sites which do not conform the known Drk SH3 domain binding motif (PxxPxR) but instead have the consensus PxxxRxxKP. Mutational analysis in vitro and in vivo provided evidence that both Drk binding sites fulfil an important function in the context of Sev and Drosophila epidermal growth factor receptor mediated signaling processes.
在发育中的果蝇眼睛中,Sevenless(Sev)受体酪氨酸激酶(RTK)的激活是R7光感受器细胞命运特化所必需的。Sevenless的女儿(Dos)是一种假定的多位点衔接蛋白,是Sev激酶的底物,并且已知与酪氨酸磷酸酶Corkscrew(Csw)相关联。Csw与Dos的结合取决于Csw的Src同源2(SH2)结构域,并且是Sev RTK信号传导的关键步骤。然而,Dos缺乏可识别的磷酸酪氨酸相互作用结构域,并且之前不清楚它是如何被招募到Sev受体的。本文表明SH2/SH3结构域衔接蛋白Drk可以提供这种联系。Drk通过其SH2结构域与自身磷酸化的Sev受体结合,而C末端的SH3结构域能够与Dos相关联。Dos上的Drk SH3结构域结合基序被定位到两个位点,这两个位点不符合已知的Drk SH3结构域结合基序(PxxPxR),而是具有共有序列PxxxRxxKP。体外和体内的突变分析提供了证据,表明在Sev和果蝇表皮生长因子受体介导的信号传导过程中,两个Drk结合位点都发挥着重要作用。