Targeting CDK7 in oncology: The avenue forward

Pharmacol Ther. 2022 Dec:240:108229. doi: 10.1016/j.pharmthera.2022.108229. Epub 2022 Jun 11.

Abstract

Cyclin-dependent kinase (CDK) 7 is best characterized for the ability to regulate biological processes, including the cell cycle and gene transcription. Abnormal CDK7 activity is observed in various tumours and represents a driving force for tumourigenesis. Therefore, CDK7 may be an appealing target for cancer treatment. Whereas, the enthusiasm for CDK7-targeted therapeutic strategy is mitigated due to the widely possessed belief that this protein is essential for normal cells. Indeed, the fact confronts the consensus. This is the first review to introduce the role of CDK7 in pan-cancers via a combined analysis of comprehensive gene information and (pre)clinical research results. We also discuss the recent advances in protein structure and summarize the understanding of mechanisms underlying CDK7 function. These endeavours highlight the pivotal roles of CDK7 in tumours and may contribute to the development of effective CDK7 inhibitors within the strategy of structure-based drug discovery for cancer therapy.

Keywords: Anti-cancer treatment; CDK7; CDK7 inhibitors; Therapeutic target.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Cycle
  • Drug Discovery
  • Humans
  • Neoplasms* / metabolism