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Updated: Jun 2, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
06:29

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Published on: July 30, 2020

Update on Aurora Kinase Targeted Therapeutics in Oncology

Myke R Green1, Joseph E Woolery, Daruka Mahadevan

  • 1Section of Hematology/Oncology, Arizona Cancer Center, Tucson, AZ.

Expert Opinion on Drug Discovery
|May 11, 2011
PubMed

Insights

Aurora kinases are crucial for cell division and cancer growth. Aurora kinase inhibitors (AKIs) are promising anti-cancer drugs, with ongoing research exploring their efficacy and resistance mechanisms in clinical trials.

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Oncology

Background:

  • Aurora A and B kinases are serine/threonine protein kinases vital for cell cycle regulation.
  • Their overexpression correlates with high proliferation rates and poor prognosis in cancers, identifying them as key therapeutic targets.
  • Targeting mitotic machinery is a validated anti-cancer strategy.

Purpose of the Study:

  • To review updated preclinical and human study results for investigational aurora kinase inhibitors (AKIs).
  • To detail Phase I data and late-breaking findings for AKIs.
  • To enable comparison of individual and class-related effects of AKIs.

Main Methods:

  • Review of preclinical and clinical studies on aurora kinase inhibitors.
  • Analysis of Phase I clinical trial data and late-breaking results.
  • Comparative analysis of AKI efficacy and effects.

Main Results:

  • Numerous small molecule AKIs have been developed and tested in vitro and in vivo.
  • Several AKIs are currently in Phase II clinical testing.
  • Data from preclinical and human studies are presented for comparison.

Conclusions:

  • Aurora kinases represent important anti-cancer targets due to their role in tumor proliferation.
  • Understanding resistance mechanisms is crucial for designing effective early-phase clinical trials and combination therapies.
  • AKIs offer a targeted and complementary approach to expand anti-cancer treatment options.

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