细胞周期蛋白依赖激酶
癌变
生物
DNA损伤
细胞周期
癌症研究
癌基因
DNA复制
激酶
抑制器
转录因子
癌症
药物发现
基因组不稳定性
细胞生物学
基因
计算生物学
生物信息学
遗传学
DNA
作者
Fatemeh Emadi,Theodosia Teo,Muhammed H. Rahaman,Shudong Wang
标识
DOI:10.1016/j.drudis.2020.09.035
摘要
Cyclin-dependent kinase (CDK) 12 engages in diversified biological functions, from transcription, post-transcriptional modification, cell cycle, and translation to cellular proliferation. Moreover, it regulates the expression of cancer-related genes involved in DNA damage response (DDR) and replication, which are responsible for maintaining genomic stability. CDK12 emerges as an oncogene or tumor suppressor in different cellular contexts, where its dysregulation results in tumorigenesis. Current CDK12 inhibitors are nonselective, which impedes the process of pharmacological target validation and drug development. Herein, we discuss the latest understanding of the biological roles of CDK12 in cancers and provide molecular analyses of CDK12 inhibitors to guide the rational design of selective inhibitors.
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