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Peptidomimetic Ligands for the Tandem SH2 Domain of the Syk Protein Involved in Signal Transduction

机译:用于信号转导的SYK蛋白的串联SH2结构域的肽肌瘤配体

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The Spleen tyrosine kinase (Syk) protein takes part in a number of receptor signaling cascades [1]. It is involved in early events after activation of e.g. the IgE-, T-cell-, B-cell- and IL-15-receptor. The role of Syk in the high affinity IgE receptor (FceRI) signaling in mast cells and basophils is shown in Fig. 1. The β- and γ-chains of FceRI contain a specific intracellular sequence called the Immunoreceptor Tyrosine based Activation Motif (IT AM). The IT AM sequence consists of Tyr-Xxx-Xxx-(Leu/Ile)-(Xxx)_(n=6-8)-Tyr-Xxx-Xxx-(Leu/Ile). in which Xxx can be any amino acid. The underlined residues comprise the binding epitopes for the tandem SH2 (tSH2) domain of Syk, when tyrosine is phosphorylated. The intervening residues (Xxx)_(n=6-8)(in FceRI n = 7) are not essential for binding.
机译:脾酪氨酸激酶(SYK)蛋白参与了许多受体信号级联[1]。它涉及激活时的早期事件。 IgE-,T细胞,B细胞和IL-15-受体。 Syk在肥大细胞和嗜碱性粒细胞中的高亲和力IgE受体(FECERI)信号传导中的SYK的作用如图1所示。Fceri的β-和γ-链含有特定的细胞内序列,称为免疫蛋白基于基于免疫蛋白酶的活化基序(它是)。它序列由Tyr-XXX-XXX-(Leu / ILE) - (XXX)_(n = 6-8)-Tyr-xxx-xxx-(Leu / Ile)组成。其中XXX可以是任何氨基酸。当酪氨酸磷酸化时,下划线的残基包含Syk的串联SH2(TSH2)结构域的结合表位。干预残留物(XXX)_(n = 6-8)(在Fceri n = 7中)对结合不是必需的。

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