August A, Sadra A, Dupont B, Hanafusa H
Laboratory of Molecular Oncology, The Rockefeller University, 1230 York Avenue, New York, NY 10021, USA.
Proc Natl Acad Sci U S A. 1997 Oct 14;94(21):11227-32. doi: 10.1073/pnas.94.21.11227.
The Tec family of tyrosine kinases are involved in signals emanating from cytokine receptors, antigen receptors, and other lymphoid cell surface receptors. One family member, ITK (inducible T cell kinase), is involved in T cell activation and can be activated by the T cell receptor and the CD28 cell surface receptor. This stimulation of tyrosine phosphorylation and activation of ITK can be mimicked by the Src family kinase Lck. We have explored the mechanism of this requirement for Src family kinases in the activation of ITK. We found that coexpression of ITK and Src results in increased membrane association, tyrosine phosphorylation and activation of ITK, which could be blocked by inhibitors of the lipid kinase phosphatidylinositol 3-kinase (PI 3-kinase) as well as overexpression of the p85 subunit of PI 3-kinase. Removal of the Pleckstrin homology domain (PH) of ITK resulted in a kinase that could no longer be induced to localize to the membrane or be activated by Src. The PH of ITK was also able to bind inositol phosphates phosphorylated at the D3 position. Membrane targeting of ITK without the PH recovered its ability to be activated by Src. These results suggest that ITK can be activated by a combination of Src and PI 3-kinase.
酪氨酸激酶的Tec家族参与细胞因子受体、抗原受体及其他淋巴细胞表面受体发出的信号。该家族成员之一,可诱导T细胞激酶(ITK),参与T细胞活化,且可被T细胞受体和CD28细胞表面受体激活。Src家族激酶Lck可模拟这种对ITK酪氨酸磷酸化及激活的刺激作用。我们探究了Src家族激酶在ITK激活过程中的这种需求机制。我们发现,ITK与Src共表达会导致ITK的膜结合增加、酪氨酸磷酸化及激活,而这可被脂质激酶磷脂酰肌醇3激酶(PI 3激酶)抑制剂以及PI 3激酶p85亚基的过表达所阻断。去除ITK的普列克底物蛋白同源结构域(PH结构域)会产生一种激酶,该激酶不再能被诱导定位于细胞膜或被Src激活。ITK的PH结构域还能够结合在D3位置磷酸化的肌醇磷酸。没有PH结构域的ITK的膜靶向恢复了其被Src激活的能力。这些结果表明,ITK可被Src和PI 3激酶共同激活。