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Chemical strategies for development of ATR inhibitors

Sabin Llona-Minguez1, Andreas Höglund1, Sylvain A Jacques1

  • 1Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, S-171 21 Stockholm, Sweden.

Expert Reviews in Molecular Medicine
|May 10, 2014
PubMed

Insights

ATR protein kinase inhibitors are crucial for genome integrity and DNA damage response. These inhibitors show promise in cancer therapy by enhancing DNA damage, especially when combined with cross-linking agents.

Area of Science:

  • Oncology
  • Molecular Biology
  • Genetics

Background:

  • ATR protein kinase is vital for maintaining genome integrity.
  • It plays a key role in coordinating DNA damage response and repair signaling pathways.
  • Inhibiting ATR disrupts signaling from stalled replication forks, increasing DNA damage.

Purpose of the Study:

  • To review existing literature on small molecule inhibitors of ATR.
  • To provide a comprehensive summary of ATR as a promising oncology target.
  • To compile research from both academic and pharmaceutical sources.

Main Methods:

  • Literature review of published research on ATR inhibitors.
  • Analysis of studies focusing on small molecule inhibitors of ATR.
  • Compilation of data from academic and pharmaceutical industry research.

Main Results:

  • ATR inhibitors prevent signaling from stalled replication forks.
  • Inhibition of ATR enhances DNA damage formation, particularly under replication stress.
  • ATR/CHK1 checkpoint inhibitors can potentiate DNA cross-linking agents.

Conclusions:

  • ATR inhibitors are a promising therapeutic strategy in oncology.
  • Clinical trials are underway for ATR inhibitors, indicating significant potential.
  • This review consolidates current knowledge on ATR inhibitors for cancer treatment.

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