Ben May Department for Cancer Research, The University of Chicago, Chicago, Illinois 60637, USA.
J Biol Chem. 2010 Apr 30;285(18):13990-4004. doi: 10.1074/jbc.M109.061309. Epub 2010 Feb 16.
Reversible ubiquitination is essential for the endocytic sorting and down-regulation of G protein-coupled receptors, such as the chemokine receptor CXCR4. The deubiquitinating enzyme AMSH has been implicated in the endocytic sorting of both G protein-coupled receptors and receptor-tyrosine kinases. Herein, we examine the role of AMSH in the regulation of CXCR4 stability and trafficking and characterize protein-protein interactions critical for this function. Loss of AMSH catalytic activity or depletion by RNAi results in increased steady-state levels of CXCR4 under basal conditions. Analysis of truncation and point mutation of AMSH reveal the importance of an RXXK motif for CXCR4 degradation. The RXXK motif of AMSH interacts with the SH3 domains of the STAM and Grb2 families of adaptor proteins with high affinity. Cells expressing a catalytically inactive mutant of AMSH show basal hyperubiquitination, but not increased degradation, of the ESCRT-0 components STAM1 and Hrs. This is dependent on the RXXK motif of AMSH. Ubiquitination of endocytic machinery modulates their activity, suggesting that AMSH may directly regulate endocytic adaptor protein function. This is reflected in CXCR4 trafficking and provides a mechanism by which AMSH specifies the fate of endocytosed receptors. Taken together, these studies implicate AMSH as a key modulator of receptor fate determination through its action on components of the endocytic machinery.
可逆泛素化对于 G 蛋白偶联受体(如趋化因子受体 CXCR4)的内吞分选和下调至关重要。去泛素化酶 AMSH 已被牵涉到 G 蛋白偶联受体和受体酪氨酸激酶的内吞分选过程中。在此,我们研究了 AMSH 在调节 CXCR4 稳定性和运输中的作用,并对这一功能至关重要的蛋白质-蛋白质相互作用进行了表征。在基础条件下,缺失 AMSH 的催化活性或通过 RNAi 耗竭会导致 CXCR4 的稳态水平增加。对 AMSH 的截断和点突变的分析揭示了 RXXK 基序对 CXCR4 降解的重要性。AMSH 的 RXXK 基序与 STAM 和 Grb2 家族的衔接蛋白的 SH3 结构域以高亲和力相互作用。表达无催化活性突变体的细胞表现出基础超泛素化,但 ESCRT-0 成分 STAM1 和 Hrs 的降解没有增加。这依赖于 AMSH 的 RXXK 基序。内吞机制的泛素化调节其活性,表明 AMSH 可能直接调节内吞衔接蛋白的功能。这反映在 CXCR4 的运输中,并提供了一种机制,通过该机制,AMSH 指定了内吞受体的命运。综上所述,这些研究表明 AMSH 通过其对内吞机制成分的作用,成为受体命运决定的关键调节剂。