Receptor tyrosine kinases (RTKs) are critical for normal cell growth, differentiation, and development, but they contribute to various pathological conditions when disrupted. Activation of RTKs stimulates a plethora of pathways, including the ubiquitylation and endocytosis of the receptor itself. Although endocytosis terminates RTK signaling, it has emerged as a requisite step in RTK activation of signaling pathways. We have discovered that the endocytic scaffolding protein intersectin (ITSN) cooperated with epidermal growth factor receptor (EGFR) in the regulation of cell growth and signaling. However, a biochemical link between ITSN and EGFR was not defined. In this study, we demonstrate that ITSN is a scaffold for the E3 ubiquitin ligase Cbl. ITSN forms a complex with Cbl in vivo mediated by the Src homology (SH) 3 domains binding to the Pro-rich COOH terminus of Cbl. This interaction stimulates the ubiquitylation and degradation of the activated EGFR. Furthermore, silencing ITSN by RNA interference attenuated EGFR internalization as well as activation of the extracellular signal-regulated kinasemitogen-activated protein kinase pathway, thereby demonstrating the importance of ITSN in EGFR function. Given the cooperativity between ITSN and additional RTKs, these results point to an important evolutionarily conserved, regulatory role for ITSN in RTK function that is necessary for both signaling from receptors as well as the ultimate termination of receptor signaling.

译文

受体酪氨酸激酶(RTKs)对于正常细胞的生长,分化和发育至关重要,但是当它们被破坏时,它们会导致各种病理状况。 RTK的激活刺激了许多途径,包括受体自身的泛素化和内吞作用。尽管内吞作用终止了RTK信号传导,但它已成为RTK激活信号通路的必要步骤。我们已经发现,内吞支架蛋白intersectin(ITSN)与表皮生长因子受体(EGFR)协同调节细胞生长和信号传导。但是,尚未定义ITSN和EGFR之间的生化联系。在这项研究中,我们证明了ITSN是E3泛素连接酶Cbl的支架。 ITSN在体内与Cbl形成复合物,该复合物是通过与Cbl富含Pro的COOH末端结合的Src同源性(SH)3结构域介导的。这种相互作用刺激了活化的EGFR的泛素化和降解。此外,通过RNA干扰使ITSN沉默可以减弱EGFR的内在化以及细胞外信号调节激酶有丝分裂原激活的蛋白激酶途径的激活,从而证明了ITSN在EGFR功能中的重要性。考虑到ITSN和其他RTK之间的协作性,这些结果表明ITSN在RTK功能中具有重要的进化保守的调节作用,这对于受体的信号传导以及受体信号传导的最终终止都是必需的。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录