Center for Vascular and Inflammatory Diseases, University of Maryland Baltimore, Baltimore, Maryland 21201, USA.
J Biol Chem. 2012 Sep 14;287(38):31948-61. doi: 10.1074/jbc.M112.348896. Epub 2012 Jul 24.
Previously, we demonstrated that the γC subunit of type I IL-4 receptor was required for robust tyrosine phosphorylation of the downstream adapter protein, IRS-2, correlating with the expression of genes (ArgI, Retnla, and Chi3l3) characteristic of alternatively activated macrophages. We located an I4R-like motif (IRS-2 docking sequence) in the γC cytoplasmic domain but not in the IL-13Rα1. Thus, we predicted that the γC tail directed enhanced IRS-2 phosphorylation. To test this, IL-4 signaling responses were examined in a mutant of the key I4R motif tyrosine residue (Y325F) and different γC truncation mutants (γ285, γ308, γ318, γ323, and γFULL LENGTH (FL)) co-expressed in L-cells or CHO cells with wild-type (WT) IL-4Rα. Surprisingly, IRS-1 phosphorylation was not diminished in Y325F L-cell mutants suggesting Tyr-325 was not required for the robust insulin receptor substrate response. IRS-2, STAT6, and JAK3 phosphorylation was observed in CHO cells expressing γ323 and γFL but not in γ318 and γ285 mutants. In addition, when CHO cells expressed γ318, γ323, or γFL with IL-2Rβ, IL-2 induced phospho-STAT5 only in the γ323 and γFL clones. Our data suggest that a smaller (5 amino acid) interval than previously determined is necessary for JAK3 activation/γC-mediated signaling in response to IL-4 and IL-2. Chimeric receptor chains of the γC tail fused to the IL-13Rα1 extracellular and transmembrane domain did not elicit robust IRS-2 phosphorylation in response to IL-13 suggesting that the extracellular/transmembrane domains of the IL-4/IL-13 receptor, not the cytoplasmic domains, control signaling efficiency. Understanding this pathway fully will lead to rational drug design for allergic disease.
先前,我们证明了 I 型 IL-4 受体的 γC 亚基对于下游衔接蛋白 IRS-2 的强烈酪氨酸磷酸化是必需的,这与替代激活的巨噬细胞特征基因(ArgI、Retnla 和 Chi3l3)的表达相关。我们在 γC 胞质结构域中发现了一个 I4R 样基序(IRS-2 对接序列),但在 IL-13Rα1 中没有发现。因此,我们预测 γC 尾部会引导 IRS-2 磷酸化增强。为了验证这一点,我们在 L 细胞或 CHO 细胞中与野生型(WT)IL-4Rα共表达关键 I4R 基序酪氨酸残基(Y325F)和不同 γC 截断突变体(γ285、γ308、γ318、γ323 和 γFULL LENGTH(FL))的突变体中检查了 IL-4 信号转导反应。令人惊讶的是,Y325F L 细胞突变体中 IRS-1 的磷酸化没有减少,这表明 Tyr-325 对于胰岛素受体底物的强烈反应不是必需的。在表达 γ323 和 γFL 的 CHO 细胞中观察到 IRS-2、STAT6 和 JAK3 的磷酸化,但在 γ318 和 γ285 突变体中没有观察到。此外,当 CHO 细胞表达 γ318、γ323 或 γFL 与 IL-2Rβ 时,IL-2 仅在 γ323 和 γFL 克隆中诱导磷酸化 STAT5。我们的数据表明,与之前确定的相比,更小的(5 个氨基酸)间隔对于 JAK3 激活/γC 介导的对 IL-4 和 IL-2 的信号转导是必需的。与 IL-13Rα1 的细胞外和跨膜结构域融合的 γC 尾部嵌合受体链不会引发对 IL-13 的强烈 IRS-2 磷酸化,这表明 IL-4/IL-13 受体的细胞外/跨膜结构域而不是细胞质结构域控制信号转导效率。充分了解这一途径将导致过敏疾病的合理药物设计。