Tyrosine phosphorylation of the nicotinic acetylcholine receptor (AChR) is associated with an altered rate of receptor desensitization and also may play a role in agrin-induced receptor clustering. We have demonstrated a previously unsuspected interaction between Torpedo AChR and the adaptor protein Grb2. The binding is mediated by the Src homology 2 (SH2) domain of Grb2 and the tyrosine-phosphorylated delta subunit of the AChR. Dephosphorylation of the delta subunit abolishes Grb2 binding. A cytoplasmic domain of the delta subunit contains a binding motif (pYXNX) for the SH2 domain of Grb2. Indeed, a phosphopeptide corresponding to this region of the delta subunit binds to Grb2 SH2 fusion proteins with relatively high affinity, whereas a peptide lacking phosphorylation on tyrosine exhibits no binding. Grb2 is colocalized with the AChR on the innervated face of Torpedo electrocytes. Furthermore, Grb2 specifically copurifies with AChR solubilized from postsynaptic membranes. These data suggest a novel role for tyrosine phosphorylation of the AChR in the initiation of a Grb2-mediated signaling cascade at the postsynaptic membrane.

译文

烟碱样乙酰胆碱受体(AChR)的酪氨酸磷酸化与受体脱敏率的改变有关,也可能在凝集素诱导的受体簇中起作用。我们已经证明了鱼雷AChR和衔接蛋白Grb2之间以前没有想到的相互作用。结合是由Grb2的Src同源2(SH2)域和AChR的酪氨酸磷酸化的δ亚基介导的。 δ亚基的去磷酸化消除了Grb2结合。 δ亚基的胞质结构域包含Grb2的SH2结构域的结合基序(pYXNX)。实际上,对应于δ亚基的该区域的磷酸肽以相对高的亲和力结合到Grb2 SH2融合蛋白上,而在酪氨酸上缺乏磷酸化的肽则没有结合。 Grb2与AChR在鱼雷电池的神经支配面上共定位。此外,Grb2与从突触后膜溶解的AChR特异共纯化。这些数据表明,AChR的酪氨酸磷酸化在突触后膜的Grb2介导的信号级联反应的起始中起着新的作用。

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