CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?,Journal of Medicinal Chemistry

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CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-03-09 , DOI: 10.1021/acs.jmedchem.9b01985
Sarah Diab ₁ , Mingfeng Yu ₂ , Shudong Wang ₂

Affiliation

Cyclin-dependent kinase (CDK) 7 has a unique functional repertoire by virtue of its dual role in transcription and cell cycle progression. Whereas CDK7 is ubiquitously expressed in various types of cancer, its downregulation leads to reduced cell proliferation. Importantly, it is now agreed that targeting transcription selectively limits the synthesis of mRNAs involved in tumor growth without causing an outage of transcription of housekeeping genes. Thus, CDK7 has been considered as a viable therapeutic target in cancer. Indeed, the development of CDK7 inhibitors has gained huge momentum with two molecules, CT7001 and SY-1365, currently under clinical development. Herein, we discuss the latest understanding of the role of CDK7 in cancer cells and provide an overview of the pharmacophores of CDK7 inhibitors, their efficacy in various cancer models, and their clinical development.

中文翻译：

癌症治疗中的CDK7抑制剂：成功的甜味？

细胞周期蛋白依赖性激酶（CDK）7由于其在转录和细胞周期进程中的双重作用而具有独特的功能库。CDK7在各种类型的癌症中普遍表达，而CDK7的下调导致细胞增殖减少。重要的是，现在已经达成共识，靶向转录选择性地限制了参与肿瘤生长的mRNA的合成，而不会引起管家基因转录的中断。因此，CDK7被认为是癌症中可行的治疗靶标。实际上，CDK7抑制剂的开发已经获得了巨大的发展动力，目前正在临床开发中的两个分子是CT7001和SY-1365。在此，我们讨论了CDK7在癌细胞中的作用的最新理解，并概述了CDK7抑制剂的药效基团，它们在各种癌症模型中的功效，

更新日期：2020-03-09

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