转录因子
计算生物学
抄写(语言学)
生物
小分子
生物信息学
遗传学
基因
语言学
哲学
作者
Huarui Cui,Morgan Stilgenbauer,Angela N. Koehler
出处
期刊:Annual review of cancer biology
[Annual Reviews]
日期:2024-01-11
卷期号:8 (1)
标识
DOI:10.1146/annurev-cancerbio-062722-012209
摘要
Dysregulated transcription factor activity is a defining feature of various cancer types. As such, targeting oncogenic transcriptional dependency has long been pursued as a potential therapeutic approach. However, transcription factors have historically been deemed as undruggable targets due to their highly disordered structures and lack of well-defined binding pockets. Nevertheless, interest in their pharmacologic inhibition and destruction has not dwindled in recent years. Here, we discuss new small-molecule-based approaches to target various transcription factors. Ligands with different mechanisms of action, such as inhibitors, molecular glue degraders, and proteolysis targeting chimeras, have recently seen success preclinically and clinically. We review how these strategies overcome the challenges presented by targeting transcription factors. Expected final online publication date for the Annual Review of Cancer Biology, Volume 8 is April 2024. Please see http://www.annualreviews.org/page/journal/pubdates for revised estimates.
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