Protein Kinase Inhibitor Peptide as a Tool to Specifically Inhibit Protein Kinase A.

Protein Kinase Inhibitor Peptide as a Tool to Specifically Inhibit Protein Kinase A.
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DOI:
10.3389/fphys.2020.574030
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发表时间:
2020
影响因子:
4
通讯作者:
Chen X
Chen X
中科院分区:
医学2区
文献类型:
--
作者:
Liu C;Ke P;Zhang J;Zhang X;Chen X

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蛋白激酶家族在细胞代谢、分裂、增殖、转录、运动和生存等几乎所有的细胞功能方面都发挥着关键作用。蛋白激酶A(PKA)由环磷酸腺苷(CAMP)激活,广泛分布于全身各系统和组织,与多种疾病的发生发展密切相关。抑制PKA的激活是研究PKA功能的基础。蛋白激酶抑制肽(PKI)是一种高效、耐热、特异的PKA抑制剂。已有研究表明,PKI可以阻断PKA介导的磷酸化酶激活。从那时起,研究人员对PKI有了大量的了解。PKI被认为是最有效、最特异的抑制PKA的方法,并被广泛应用于相关研究。在这篇综述中,我们将首先介绍有关PKA激活的知识以及PKI抑制PKA作用的相关机制。然后,我们将比较PKI介导的PKA抑制和几种流行的PKA抑制方法。
The protein kinase enzyme family plays a pivotal role in almost every aspect of cellular function, including cellular metabolism, division, proliferation, transcription, movement, and survival. Protein kinase A (PKA), whose activation is triggered by cyclic adenosine monophosphate (cAMP), is widely distributed in various systems and tissues throughout the body and highly related to pathogenesis and progression of various kinds of diseases. The inhibition of PKA activation is essential for the study of PKA functions. Protein kinase inhibitor peptide (PKI) is a potent, heat-stable, and specific PKA inhibitor. It has been demonstrated that PKI can block PKA-mediated phosphorylase activation. Since then, researchers have a lot of knowledge about PKI. PKI is considered to be the most effective and specific method to inhibit PKA and is widely used in related research. In this review, we will first introduce the knowledge on the activation of PKA and mechanisms related on the inhibitory effects of PKI on PKA. Then, we will compare PKI-mediated PKA inhibition vs. several popular methods of PKA inhibition.
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