VerPlank Jordan J S, Goldberg Alfred L
Harvard Medical School, Boston, MA 02115, U.S.A.
Biochem J. 2017 Sep 24;474(19):3355-3371. doi: 10.1042/BCJ20160809.
The ubiquitin proteasome system degrades the great majority of proteins in mammalian cells. Countless studies have described how ubiquitination promotes the selective degradation of different cell proteins. However, there is a small but the growing literature that protein half-lives can also be regulated by post-translational modifications of the 26S proteasome. The present study reviews the ability of several kinases to alter proteasome function through subunit phosphorylation. For example, PKA (protein kinase A) and DYRK2 (dual-specificity tyrosine-regulated kinase 2) stimulate the proteasome's ability to degrade ubiquitinated proteins, peptides, and adenosine triphosphate, while one kinase, ASK1 (apoptosis signal-regulating kinase 1), inhibits proteasome function during apoptosis. Proteasome phosphorylation is likely to be important in regulating protein degradation because it occurs downstream from many hormones and neurotransmitters, in conditions that raise cyclic adenosine monophosphate or cyclic guanosine monophosphate levels, after calcium influx following synaptic depolarization, and during phases of the cell cycle. Beyond its physiological importance, pharmacological manipulation of proteasome phosphorylation has the potential to combat various diseases. Inhibitors of phosphodiesterases by activating PKA or PKG (protein kinase G) can stimulate proteasomal degradation of misfolded proteins that cause neurodegenerative or myocardial diseases and even reduce the associated pathology in mouse models. These observations are promising since in many proteotoxic diseases, aggregation-prone proteins impair proteasome function, and disrupt protein homeostasis. Conversely, preventing subunit phosphorylation by DYRK2 slows cell cycle progression and tumor growth. However, further research is essential to determine how phosphorylation of different subunits by these (or other) kinases alters the properties of this complex molecular machine and thus influence protein degradation rates.
泛素蛋白酶体系统降解哺乳动物细胞中的绝大多数蛋白质。无数研究描述了泛素化如何促进不同细胞蛋白质的选择性降解。然而,有一小部分但数量不断增加的文献表明,蛋白质半衰期也可通过26S蛋白酶体的翻译后修饰来调节。本研究综述了几种激酶通过亚基磷酸化改变蛋白酶体功能的能力。例如,蛋白激酶A(PKA)和双特异性酪氨酸调节激酶2(DYRK2)可刺激蛋白酶体降解泛素化蛋白质、肽和三磷酸腺苷的能力,而一种激酶,即凋亡信号调节激酶1(ASK1),在细胞凋亡过程中抑制蛋白酶体功能。蛋白酶体磷酸化在调节蛋白质降解中可能很重要,因为它发生在许多激素和神经递质的下游,在环磷酸腺苷或环磷酸鸟苷水平升高的情况下,在突触去极化后钙内流期间,以及在细胞周期的各个阶段。除了其生理重要性外,对蛋白酶体磷酸化的药理学操纵有可能对抗各种疾病。通过激活PKA或蛋白激酶G(PKG)的磷酸二酯酶抑制剂可刺激导致神经退行性或心肌疾病的错误折叠蛋白质的蛋白酶体降解,甚至可减轻小鼠模型中的相关病理变化。这些观察结果很有前景,因为在许多蛋白毒性疾病中,易于聚集的蛋白质会损害蛋白酶体功能,并破坏蛋白质稳态。相反,阻止DYRK2介导的亚基磷酸化会减缓细胞周期进程和肿瘤生长。然而,进一步的研究对于确定这些(或其他)激酶对不同亚基的磷酸化如何改变这一复杂分子机器的特性,进而影响蛋白质降解速率至关重要。