Suzuki-Inoue Katsue, Tulasne David, Shen Yang, Bori-Sanz Teresa, Inoue Osamu, Jung Stephanie M, Moroi Masaaki, Andrews Robert K, Berndt Michael C, Watson Steve P
Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, United Kingdom.
J Biol Chem. 2002 Jun 14;277(24):21561-6. doi: 10.1074/jbc.M201012200. Epub 2002 Apr 9.
The glycoprotein VI (GPVI)-Fc receptor (FcR) gamma-chain complex, a key activatory receptor for collagen on platelet surface membranes, is constitutively associated with the Src family kinases Fyn and Lyn. Molecular cloning of GPVI has revealed the presence of a proline-rich domain in the sequence of GPVI cytoplasmic tail which has the consensus for interaction with the Src homology 3 (SH3) domains of Fyn and Lyn. A series of in vitro experiments demonstrated the ability of the SH3 domains of both Src kinases to bind the proline-rich domain of GPVI. Furthermore, depletion of the proline-rich domain in GPVI (Pro(-)-GPVI) prevented binding of Fyn and Lyn and markedly reduced phosphorylation of FcR gamma-chain in transiently transfected COS-7 cells, but did not affect the association of the gamma-chain with GPVI. Jurkat cells stably transfected with wild type GPVI show robust increases in tyrosine phosphorylation and intracellular Ca2+ in response to the snake venom convulxin that targets GPVI. Importantly, convulxin is not able to activate cells transfected with Pro(-)-GPVI, even though the association with the immunoreceptor tyrosine-based activation motif-containing chains is maintained. These findings demonstrate that the proline-rich domain of GPVI mediates the association with Fyn/Lyn via their SH3 domain and that this interaction initiates activation signals through GPVI.
糖蛋白VI(GPVI)-Fc受体(FcR)γ链复合物是血小板表面膜上胶原蛋白的关键激活受体,它与Src家族激酶Fyn和Lyn组成性结合。GPVI的分子克隆显示其胞质尾序列中存在富含脯氨酸的结构域,该结构域具有与Fyn和Lyn的Src同源3(SH3)结构域相互作用的共有序列。一系列体外实验证明了两种Src激酶的SH3结构域均能结合GPVI富含脯氨酸的结构域。此外,GPVI中富含脯氨酸结构域的缺失(Pro(-)-GPVI)可阻止Fyn和Lyn的结合,并显著降低瞬时转染的COS-7细胞中FcRγ链的磷酸化,但不影响γ链与GPVI的结合。稳定转染野生型GPVI的Jurkat细胞在受到靶向GPVI的蛇毒convulxin刺激时,酪氨酸磷酸化和细胞内Ca2+水平显著升高。重要的是,尽管与含免疫受体酪氨酸激活基序的链的结合得以维持,但convulxin无法激活转染了Pro(-)-GPVI的细胞。这些发现表明,GPVI富含脯氨酸的结构域通过其SH3结构域介导与Fyn/Lyn的结合,并通过GPVI启动激活信号。