Related Experiment Video

Updated: Aug 30, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Inhibitors of the G2 DNA damage checkpoint and their potential for cancer therapy

Hilary J Anderson1, Raymond J Andersen, Michel Roberge

  • 1Department of Biochemistry and Molecular Biology, University of British Columbia, Vancouver, BC, V6T 1Z3, Canada.

Progress in Cell Cycle Research
|November 5, 2003
PubMed

Insights

Cancer cells often have faulty G1 checkpoints but impaired G2 checkpoints. G2 checkpoint inhibitors can sensitize these cancer cells to DNA-damaging treatments, offering potential cancer therapy strategies.

Area of Science:

  • Cellular biology
  • Molecular oncology
  • Cancer therapeutics

Background:

  • Cell cycle checkpoints, including G1 and G2, are crucial for DNA repair and genomic stability.
  • Most cancer cells exhibit a non-functional G1 checkpoint due to p53 inactivation.
  • Cancer cells retain a G2 checkpoint, albeit often impaired.

Purpose of the Study:

  • To review G2 checkpoint inhibitors for cancer therapy.
  • To discuss their chemical structures, targets, and cellular effects.
  • To evaluate their therapeutic potential in combination treatments.

Main Methods:

  • Review of literature on cell-based and target-directed screens for checkpoint inhibitors.
  • Analysis of identified G2 checkpoint inhibitors.
  • Discussion of their biochemical targets and cellular mechanisms.

Main Results:

  • Several G2 checkpoint inhibitors have been identified through various screening methods.
  • These inhibitors demonstrate potential in sensitizing cancer cells with inactive p53 to DNA-damaging agents.
  • Inhibitors target specific pathways involved in G2/M transition and DNA damage response.

Conclusions:

  • G2 checkpoint inhibitors represent a promising strategy for cancer therapy, particularly for tumors with p53 deficiencies.
  • Combination therapy with DNA-damaging drugs or radiation may enhance treatment efficacy.
  • Further research into the chemical structures, targets, and clinical applications of these inhibitors is warranted.

More Related Videos

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics06:00

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics

Published on: May 14, 2016

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology07:04

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology

Published on: May 2, 2025

Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Negative Regulator Molecules01:23

Negative Regulator Molecules

Positive regulators allow a cell to advance through cell cycle checkpoints. Negative regulators have an equally important role as they terminate a cell’s progression through the cell cycle—or pause it—until the cell meets specific criteria.
DNA Damage can Stall the Cell Cycle02:36

DNA Damage can Stall the Cell Cycle

In response to DNA damage, cells can pause the cell cycle to assess and repair the breaks. However, the cell must check the DNA at certain critical stages during the cell cycle. If the cell cycle pauses before DNA replication, the cells will contain twice the amount of DNA. On the other hand, if cells arrest after DNA replication but before mitosis, they will contain four times the normal amount of DNA. With a host of specialized proteins at their disposal,cells must use the right protein at...
DNA Damage Can Stall the Cell Cycle02:36

DNA Damage Can Stall the Cell Cycle

In response to DNA damage, cells can pause the cell cycle to assess and repair the breaks. However, the cell must check the DNA at certain critical stages during the cell cycle. If the cell cycle pauses before DNA replication, the cells will contain twice the amount of DNA. On the other hand, if cells arrest after DNA replication but before mitosis, they will contain four times the normal amount of DNA. With a host of specialized proteins at their disposal,cells must use the right protein at...
Inhibitors of Bacterial DNA Synthesis01:28

Inhibitors of Bacterial DNA Synthesis

Bacterial pathogens depend on precise and efficient DNA replication to sustain infection. Two type II topoisomerases—DNA gyrase and topoisomerase IV—are critical to this process, as they resolve DNA supercoiling and unlink chromosomes during replication. Fluoroquinolones, synthetic derivatives of quinolones, exploit this mechanism by stabilizing the transient DNA–enzyme cleavage complex, preventing strand religation, and causing lethal double-strand breaks. These antibiotics are selectively...