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Progress in the development of selective inhibitors of Aurora kinases

Andrew Mortlock1, Nicholas J Keen, Frederic H Jung

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

Current Topics in Medicinal Chemistry
|April 28, 2005
PubMed

Insights

Errors in cell division (mitosis) contribute to cancer's genetic instability. Aurora kinase inhibitors are emerging as novel anti-cancer drugs, with medicinal chemistry driving their development.

Area of Science:

  • Molecular Biology
  • Oncology
  • Medicinal Chemistry

Background:

  • Mitotic errors are a primary driver of genetic instability in cancer.
  • Proteins regulating mitosis are often dysregulated in tumor cells, presenting therapeutic targets.
  • Aurora kinases are key regulators of mitosis and are 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 role of Aurora kinases as potential anti-cancer drug targets.
  • To discuss the current landscape of Aurora kinase inhibitors in clinical development.

Main Methods:

  • Literature review focusing on medicinal chemistry contributions.
  • Analysis of small molecule inhibitors targeting Aurora kinase family.
  • Examination of the role of Aurora kinases in cell cycle regulation and cancer.

Main Results:

  • Aberrant expression of mitotic regulators, including Aurora kinases, is common in cancer.
  • Small molecule inhibitors targeting Aurora kinases show promise as anti-cancer agents.
  • Significant medicinal chemistry efforts have yielded a broad range of inhibitors.

Conclusions:

  • Aurora kinases are validated targets for anti-cancer drug development.
  • Medicinal chemistry has been crucial in advancing Aurora kinase inhibitors towards clinical application.
  • Further development of these inhibitors holds potential for novel cancer therapies.

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