Targeting cell cycle regulation via the G2-M checkpoint for synthetic lethality in melanoma

Cell Cycle. 2021 Jun;20(11):1041-1051. doi: 10.1080/15384101.2021.1922806. Epub 2021 May 9.

Abstract

Disruption of cell cycle checkpoints has been well established as a hallmark of cancer. In particular, the G1-S transition mediated by the cyclin D-cyclin-dependent kinase 4/6 (CDK4/6) pathway is dysregulated in more than 90% of melanoma cases. Therefore, tumor cells mainly rely on the G2-M checkpoint to halt the cell cycle in order to repair DNA damage. Here, we review the promising method of cell cycle-mediated synthetic lethality for melanoma treatment, which entails exploiting somatically acquired mutations in the G1-S transition with inhibitors of the G2-M transition in order to specifically kill melanoma cells. The idea stems from the theory that melanoma cells lacking G1-S checkpoints are particularly vulnerable to mitotic catastrophe when presented with G2-M checkpoint inhibition in addition to DNA damage, whereas normal cells with intact G1-S checkpoints should theoretically be spared. This review explores the link between cell cycle dysregulation and synthetic lethality in melanoma cells and discusses potential future applications for this treatment.

Keywords: CHK1; G1-S transition; G2-M transition; WEE1; cell cycle checkpoint; melanoma; synthetic lethality.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Cell Cycle Checkpoints / drug effects
  • Cell Cycle Checkpoints / genetics
  • Checkpoint Kinase 1 / genetics
  • DNA Damage / drug effects
  • DNA Damage / genetics
  • G2 Phase Cell Cycle Checkpoints / drug effects
  • G2 Phase Cell Cycle Checkpoints / genetics*
  • Humans
  • Immune Checkpoint Inhibitors / pharmacology
  • Immune Checkpoint Inhibitors / therapeutic use
  • Melanoma / drug therapy
  • Melanoma / genetics*
  • Skin Neoplasms / drug therapy
  • Skin Neoplasms / genetics*
  • Synthetic Lethal Mutations / drug effects
  • Synthetic Lethal Mutations / genetics*

Substances

  • Antineoplastic Agents
  • Immune Checkpoint Inhibitors
  • CHEK1 protein, human
  • Checkpoint Kinase 1