Targeting CDK7 in oncology: The avenue forward.
Targeting CDK7 in oncology: The avenue forward.
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DOI：
10.1016/j.pharmthera.2022.108229
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发表时间：
2022-06
影响因子：
13.5
通讯作者：
Zhi-Mei Li;Guan-yu Liu;Ya Gao;M. Zhao
中科院分区：
文献类型：
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作者：
Zhi-Mei Li;Guan-yu Liu;Ya Gao;M. Zhao
细胞周期蛋白依赖性激酶（CDK）7的最大特点是能够调节生物过程，包括细胞周期和基因转录。在各种肿瘤中观察到异常的CDK7活性，并代表肿瘤发生的驱动力。因此，CDK7可能是一个有吸引力的癌症治疗靶点。然而，对CDK7靶向治疗策略的热情由于普遍认为这种蛋白质对正常细胞是必需的而有所减弱。事实上，这一事实与共识相悖。这是第一篇通过综合基因信息和（前）临床研究结果的综合分析介绍CDK7在泛癌症中的作用的综述。我们还讨论了蛋白质结构的最新进展，并总结了对CDK7功能机制的理解。这些努力突出了CDK7在肿瘤中的关键作用，并可能有助于在基于结构的癌症治疗药物发现策略中开发有效的CDK7抑制剂。
Cyclin-dependent kinase (CDK) 7 is best characterized for the ability to regulate biological processes, including the cell cycle and gene transcription. Abnormal CDK7 activity is observed in various tumours and represents a driving force for tumourigenesis. Therefore, CDK7 may be an appealing target for cancer treatment. Whereas, the enthusiasm for CDK7-targeted therapeutic strategy is mitigated due to the widely possessed belief that this protein is essential for normal cells. Indeed, the fact confronts the consensus. This is the first review to introduce the role of CDK7 in pan-cancers via a combined analysis of comprehensive gene information and (pre)clinical research results. We also discuss the recent advances in protein structure and summarize the understanding of mechanisms underlying CDK7 function. These endeavours highlight the pivotal roles of CDK7 in tumours and may contribute to the development of effective CDK7 inhibitors within the strategy of structure-based drug discovery for cancer therapy.