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Progress in the development of selective inhibitors of aurora kinases

Andrew A Mortlock1, Nicholas J Keen, Frederic H Jung

  • 1Cancer and Infection Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK. andrew.mortlock@astrazeneca.com

Current Topics in Medicinal Chemistry
|August 17, 2005
PubMed

Insights

Errors in mitosis cause genetic instability in cancer. Aurora kinase inhibitors are promising anti-cancer drugs, with medicinal chemistry driving their development for cancer treatment.

Area of Science:

  • Molecular Biology
  • Oncology
  • Medicinal Chemistry

Background:

  • Mitotic errors are a key driver of cancer-related genetic instability.
  • Proteins regulating mitosis are often dysregulated in tumor cells, presenting therapeutic targets.
  • Aurora kinases are crucial mitotic regulators implicated in cancer development.

Purpose of the Study:

  • To review the medicinal chemistry efforts in developing small molecule inhibitors targeting Aurora kinases.
  • To highlight the therapeutic potential of Aurora kinase inhibitors in cancer treatment.

Main Methods:

  • Literature review of medicinal chemistry studies on Aurora kinase inhibitors.
  • Analysis of the role of Aurora kinases in cell cycle regulation and cancer.
  • Examination of the development status of small molecule inhibitors in clinical trials.

Main Results:

  • Aberrant expression of mitotic regulators, including Aurora kinases, is common in cancer.
  • Small molecule inhibitors targeting Aurora kinases show significant therapeutic promise.
  • Medicinal chemistry has been instrumental in creating a diverse range of Aurora kinase inhibitors.

Conclusions:

  • Aurora kinases are validated targets for novel anti-cancer drug development.
  • The ongoing clinical development of Aurora kinase inhibitors underscores their therapeutic potential.
  • Continued medicinal chemistry research is vital for advancing Aurora kinase inhibitor-based cancer therapies.

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