Related Experiment Video
Updated: Jun 1, 2026
Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
Checkpoint kinase inhibitors: a patent review (2009 - 2010)
Michael Lainchbury1, Ian Collins
1The Institute of Cancer Research, Cancer Research UK Cancer Therapeutics Unit, Haddow Laboratories, Sutton, Surrey, UK. michael.lainchbury@icr.ac.uk
Introduction:
Cells that suffer DNA damage activate the checkpoint kinases CHK1 and CHK2, which signal to initiate repair processes, limit cell-cycle progression and prevent cell replication, until the damaged DNA is repaired. Due to their potential application as novel anticancer therapies, inhibitors of CHK1 and CHK2 have become the focus of numerous drug discovery projects.
Areas Covered:
This patent review examines the chemical structures and biological activities of recently reported CHK1 and CHK2 inhibitors. The chemical abstract and patent databases SciFinder and esp@cenet were used to locate patent applications that were published between September 2008 and December 2010, claiming chemical structures for use as CHK1 or CHK2 inhibitors.
Expert Opinion:
This is an exciting time for checkpoint kinase inhibitors, with several currently in Phase I or II clinical trials. Many of the CHK1 inhibitors contained within this patent review have shown preclinical efficacy in combination with DNA-damaging chemotherapies. CHK1 inhibitors have recently been demonstrated to be efficacious as single agents in preclinical models of tumors with constitutive activation of CHK1 or high intrinsic DNA damage due to replication stress. The level of newly published patent applications covering CHK1 and CHK2 inhibitors remains high and a diverse range of scaffolds has been claimed.
Insights
Checkpoint kinase inhibitors targeting CHK1 and CHK2 are promising anticancer therapies. Recent patents reveal diverse chemical structures with preclinical efficacy, some advancing to clinical trials.
Area of Science:
- Oncology
- Molecular Biology
- Medicinal Chemistry
Background:
- DNA damage triggers checkpoint kinases CHK1 and CHK2.
- These kinases are crucial for DNA repair and cell cycle regulation.
- Inhibitors of CHK1/CHK2 are investigated as novel anticancer agents.
Purpose of the Study:
- To review recent patent literature on CHK1 and CHK2 inhibitors.
- To analyze chemical structures and biological activities of these inhibitors.
Main Methods:
- Patent review focusing on applications published between September 2008 and December 2010.
- Searches conducted using SciFinder and esp@cenet databases.
- Identification of patents claiming chemical structures for CHK1 or CHK2 inhibition.
Main Results:
- A high volume of patent applications for CHK1 and CHK2 inhibitors were published.
- Diverse chemical scaffolds have been claimed in these patents.
- Many CHK1 inhibitors demonstrated preclinical efficacy, particularly in combination therapies.
Conclusions:
- Checkpoint kinase inhibitors represent an active area of drug discovery.
- Several CHK1 inhibitors are in early-stage clinical trials.
- CHK1 inhibitors show potential as single agents in specific cancer models and in combination treatments.
Related Concept Videos
02:34Inhibition of Cdk Activity
02:34Inhibition of CDK Activity
01:15Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions
02:54Protein Kinases and Phosphatases
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
02:54Protein Kinases and Phosphatases
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
02:15M-Cdk Drives Transition Into Mitosis
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...