posted on 2020-03-19, 19:18authored bySarah Diab, Mingfeng Yu, Shudong Wang
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.