Reality CHEK: Understanding the biology and clinical potential of CHK1

Cancer Lett. 2021 Jan 28:497:202-211. doi: 10.1016/j.canlet.2020.09.016. Epub 2020 Sep 28.

Abstract

The DNA damage response enables cells to cope with various stresses that threaten genomic integrity. A critical component of this response is the serine/threonine kinase CHK1 which is encoded by the CHEK1 gene. Originally identified as a regulator of the G2/M checkpoint, CHK1 has since been shown to play important roles in DNA replication, mitotic progression, DNA repair, and overall cell cycle regulation. However, the potential of CHK1 as a cancer therapy has not been realized clinically. Herein we expound our current understanding of the principal roles of CHK1 and highlight different avenues for CHK1 targeting in cancer therapy.

Keywords: CHK1; Cell cycle; DNA Damage response.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Checkpoint Kinase 1 / antagonists & inhibitors*
  • Checkpoint Kinase 1 / genetics
  • Checkpoint Kinase 1 / metabolism
  • DNA Damage
  • DNA Repair
  • Humans
  • Molecular Targeted Therapy*
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neoplasms / pathology*
  • Protein Kinase Inhibitors / pharmacology*

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Checkpoint Kinase 1