Targeting key proteins involved in transcriptional regulation for cancer therapy: Current strategies and future prospective

癌症治疗 生物 钥匙(锁) 癌症 计算生物学 医学 神经科学 生物信息学 癌症研究 内科学 生态学
作者
Haixiang Pei,Weikai Guo,Yangrui Peng,Hai Xiong,Yihua Chen
出处
期刊:Medicinal Research Reviews [Wiley]
卷期号:42 (4): 1607-1660 被引量:30
标识
DOI:10.1002/med.21886
摘要

The key proteins involved in transcriptional regulation play convergent roles in cellular homeostasis, and their dysfunction mediates aberrant gene expressions that underline the hallmarks of tumorigenesis. As tumor progression is dependent on such abnormal regulation of transcription, it is important to discover novel chemical entities as antitumor drugs that target key tumor-associated proteins involved in transcriptional regulation. Despite most key proteins (especially transcription factors) involved in transcriptional regulation are historically recognized as undruggable targets, multiple targeting approaches at diverse levels of transcriptional regulation, such as epigenetic intervention, inhibition of DNA-binding of transcriptional factors, and inhibition of the protein-protein interactions (PPIs), have been established in preclinically or clinically studies. In addition, several new approaches have recently been described, such as targeting proteasomal degradation and eliciting synthetic lethality. This review will emphasize on accentuating these developing therapeutic approaches and provide a thorough conspectus of the drug development to target key proteins involved in transcriptional regulation and their impact on future oncotherapy.
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