摘要
细胞周期蛋白依赖性激酶 (CDK) 包括约 20 种丝氨酸/苏氨酸激酶家族,其催化活性需要称为细胞周期蛋白的调节亚基;这些酶在细胞周期和转录中发挥多种作用。 PCTAIRE 激酶 (PCTK) 是 CDK 亚家族,其特征在于共有 PSTAIRE 基序中的丝氨酸至半胱氨酸突变,参与与细胞周期蛋白的结合。该类的一个成员是 PCTK3,它有两个同种型(a 和 b),也称为 CDK18。在被细胞周期蛋白 A2 激活或被 PKA 磷酸化 Ser12 后,PCTK3 可以执行多种功能。在这些功能中,我们可以强调以下内容:膜运输中货物运输的调节、p53 响应基因、基因组完整性的调节。根据不同的研究,PCTK3功能障碍与多种疾病有关,如代谢性疾病、脑缺血、抑郁症、癌症、神经系统疾病和阿尔茨海默病等。尽管该蛋白质参与了不同的生物学事件,但我们可以说 PCTK3 受到的关注远低于其他 CDK。关于其他 CDK 的已发表文章数以千计,与 PCTK3 相关的文章不足两百篇。本综述的主要目的是介绍有关该蛋白质的选定已发表研究。与其他 CDK 相比,我们的重点是 PCTK3 的特殊性。在这里,我们概述了 PCTK3 的生物学功能,并探索其作为药物设计靶点的潜力。
关键词: CDK18、PCTAIRE 3、DNA 复制应激、转录、癌症、阿尔茨海默病、PCTK3。
Current Medicinal Chemistry
Title:Overview of PCTK3/CDK18: A Cyclin-Dependent Kinase Involved in Specific Functions in Post-Mitotic Cells
Volume: 28 Issue: 33
关键词: CDK18、PCTAIRE 3、DNA 复制应激、转录、癌症、阿尔茨海默病、PCTK3。
摘要: Cyclin-dependent kinases (CDKs) comprise a family of about 20 serine/threonine kinases whose catalytic activity requires a regulatory subunit known as cyclin; these enzymes play several roles in the cell cycle and transcription. PCTAIRE kinases (PCTKs) are a CDK subfamily, characterized by serine to cysteine mutation in the consensus PSTAIRE motif, involved in binding to the cyclin. One member of this class is PCTK3, which has two isoforms (a and b) and is also known as CDK18. After being activated by cyclin A2 or phosphorylation at Ser12 by PKA, PCTK3 can perform several functions. Among these functions, we may highlight the following: modulation of cargo transport in membrane traffic, p53-responsive gene, regulation of genome integrity. According to different studies, PCTK3 dysfunction is related to a wide range of diseases, such as metabolic diseases, cerebral ischemia, depression, cancer, neurological disorders, and Alzheimer's disease. Although this protein participates in different biological events, we may say that PCTK3 has received far less attention than other CDKs. There are thousands of published articles about other CDKs and less than two hundred articles related to PCTK3. The main objective of this review is to present the selected published studies about this protein. Our focus is on PCTK3 particularities compared to other CDKs. Here we give an overview of the biological functions of PCTK3 and explore its potential as a target for drug design.
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Cite this article as:
Overview of PCTK3/CDK18: A Cyclin-Dependent Kinase Involved in Specific Functions in Post-Mitotic Cells, Current Medicinal Chemistry 2021; 28 (33) . https://dx.doi.org/10.2174/0929867328666210329122147
DOI https://dx.doi.org/10.2174/0929867328666210329122147 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |

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