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Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
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Aurora kinase inhibitors: progress towards the clinic

Madhu Kollareddy1, Daniella Zheleva, Petr Dzubak

  • 1Laboratory of Experimental Medicine, Institute of Molecular and Translational Medicine, Palacky University, Puskinova 6, Olomouc, 77520, Czech Republic.

Investigational New Drugs
|February 22, 2012
PubMed

Insights

Aurora kinases are crucial for cell division and cancer. This review details promising Aurora kinase inhibitors in development, focusing on their action, resistance, and clinical performance as cancer therapies.

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • Aurora kinases, essential serine/threonine kinases, regulate cell division, particularly mitosis.
  • Their critical role in human biology and frequent association with cancer have established them as significant therapeutic targets.
  • Mutant alleles in Drosophila melanogaster initially led to their discovery, highlighting conserved functions.

Purpose of the Study:

  • To review the characteristics and developmental status of Aurora kinase inhibitors.
  • To emphasize mechanisms of action, resistance, and clinical performance of these anticancer agents.
  • To discuss the validity of Aurora kinases as oncology targets and their future potential.

Main Methods:

  • Review of preclinical and clinical studies (Phase I and II) of Aurora kinase inhibitors.
  • Analysis of binding modes, including hydrogen bonds and noncovalent interactions within the kinase active site.
  • Examination of on/off-target toxicities and overall clinical efficacy.

Main Results:

  • Approximately 30 Aurora kinase inhibitors are in various stages of development.
  • Inhibitors share common binding interactions with the kinase hinge region.
  • Mechanisms of action and resistance are key factors influencing clinical outcomes.

Conclusions:

  • Aurora kinase inhibitors represent a promising class of anticancer agents.
  • Understanding resistance mechanisms and managing toxicities are crucial for successful clinical application.
  • Continued development and investigation are warranted to optimize their therapeutic potential in oncology.

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