文章：

转录因子作为癌症治疗的靶点

Transcription factors as targets for cancer therapy

原文发布日期：2002-10-01

DOI: 10.1038/nrc906

类型: Review Article

开放获取: 否

要点：

1. Signalling proteins, which are often mutated in cancer, change transcription patterns.
2. Many more signalling proteins are affected in cancer than transcription factors, electing transcription factors as cogent targets.
3. One or more latent cytoplasmic transcription factors (such as STATs, NF-κB, β-catenin and Notch intracellular domain (NICD)) have increased activity in most human cancers, and in many cases prevent apoptosis of cancer cells.
4. Necessary physical interaction among transcription factors and cofactors in the nucleus affords selective sites of potential drug action.
5. Should pharmacology of transcription-factor inhibition be the wave of the future? It might be difficult, but it should not be impossible.

要点翻译：

1. 在癌症中常发生突变的信号蛋白会改变转录模式。
2. 相比转录因子，更多信号蛋白在癌症中受到影响，这使得转录因子成为有效的治疗靶点。
3. 一种或多种潜在的胞质转录因子（如STATs、NF-κB、β-连环蛋白和Notch细胞内结构域NICD）在大多数人类癌症中活性增强，并在许多情况下阻止癌细胞的凋亡。
4. 转录因子与辅因子在细胞核内必要的物理相互作用，为潜在的药物作用提供了选择性位点。
5. 转录因子抑制药理学是否将成为未来趋势？这可能很困难，但并非不可能。

英文摘要：

A limited list of transcription factors are overactive in most human cancer cells, which makes them targets for the development of anticancer drugs. That they are the most direct and hopeful targets for treating cancer is proposed, and this is supported by the fact that there are many more human oncogenes in signalling pathways than there are oncogenic transcription factors. But how could specific transcription-factor activity be inhibited?

摘要翻译： 

在大多数人类癌细胞中，少数转录因子过度活跃，因此成为抗癌药物开发的靶点。有人提出，它们是治疗癌症最直接、最有希望的药物靶点；信号通路中人类癌基因的数量远多于致癌性转录因子，这一事实支持了该观点。但是，如何抑制特定转录因子的活性呢？

原文链接：

Transcription factors as targets for cancer therapy