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一种新的N端疏水基序通过泛素-蛋白酶体途径介导血清和糖皮质激素诱导激酶-1的组成型降解。

A novel N-terminal hydrophobic motif mediates constitutive degradation of serum- and glucocorticoid-induced kinase-1 by the ubiquitin-proteasome pathway.

作者信息

Bogusz Agata M, Brickley Deanna R, Pew Travis, Conzen Suzanne D

机构信息

Department of Pathology, The University of Chicago, IL, USA.

出版信息

FEBS J. 2006 Jul;273(13):2913-28. doi: 10.1111/j.1742-4658.2006.05304.x.

Abstract

Serum- and glucocorticoid-induced protein kinase-1 (SGK-1) plays a critical role in regulation of the epithelial sodium channel, ENaC. SGK-1 also shares significant catalytic domain homology with protein kinase B (PKB/AKT-1) and is a downstream effector of antiapoptotic phosphoinositide 3-kinase signaling. Steady-state levels of an active SGK-1 are tightly regulated by rapid transcriptional activation and post-translational modification including phosphorylation. We show here that endogenous SGK-1 protein is polyubiquitinated and rapidly degraded by the 26S proteasome. In contrast to other rapidly degraded kinases, neither the catalytic activity of SGK-1 nor activation site phosphorylation was required for its ubiquitin modification and degradation. Instead, SGK-1 degradation required a lysine-less six-amino-acid (amino acids 19-24) hydrophobic motif (GMVAIL) within the N-terminal domain. Deletion of amino acids 19-24 significantly increased the half-life of SGK1 and prevented its ubiquitin modification. Interestingly, this minimal region was also required for the association of SGK-1 with the endoplasmic reticulum. Ubiquitin modification and degradation of SGK-1 were increasingly inhibited by the progressive mutation of six N-terminal lysine residues surrounding the GMVAIL motif. Mutation of all six lysines to arginine did not disrupt the subcellular localization of SGK-1 despite a significant decrease in ubiquitination, implying that this modification per se was not required for targeting to the endoplasmic reticulum. These results suggest that constitutive ubiquitin-mediated degradation of SGK-1 is an important mechanism regulating its biological activity.

摘要

血清和糖皮质激素诱导蛋白激酶-1(SGK-1)在上皮钠通道ENaC的调节中起关键作用。SGK-1与蛋白激酶B(PKB/AKT-1)也具有显著的催化结构域同源性,并且是抗凋亡磷酸肌醇3激酶信号传导的下游效应器。活性SGK-1的稳态水平通过快速转录激活和包括磷酸化在内的翻译后修饰受到严格调控。我们在此表明,内源性SGK-1蛋白被多聚泛素化并被26S蛋白酶体快速降解。与其他快速降解的激酶不同,SGK-1的泛素修饰和降解既不需要其催化活性也不需要激活位点磷酸化。相反,SGK-1的降解需要N端结构域内一个无赖氨酸的六氨基酸(第19 - 24位氨基酸)疏水基序(GMVAIL)。删除第19 - 24位氨基酸显著增加了SGK1的半衰期并阻止了其泛素修饰。有趣的是,这个最小区域也是SGK-1与内质网结合所必需的。围绕GMVAIL基序的六个N端赖氨酸残基的逐步突变越来越抑制SGK-1的泛素修饰和降解。尽管泛素化显著减少,但将所有六个赖氨酸突变为精氨酸并未破坏SGK-1的亚细胞定位,这意味着这种修饰本身并非靶向内质网所必需。这些结果表明,SGK-1的组成型泛素介导降解是调节其生物学活性的重要机制。

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