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Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
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Aurora A and B kinases as targets for cancer: will they be selective for tumors?

Nick Matthews1, Cristina Visintin, Basil Hartzoulakis

  • 1Inploid Ltd, Oxford BioBusiness Centre, Littlemore Park, Oxford, OX4 4SS, UK. nick@inploid.wanadoo.co.uk

Expert Review of Anticancer Therapy
|December 27, 2005
PubMed

Insights

Aurora kinases are key regulators of the cell cycle and promising cancer targets. This review covers current inhibitors, their structures, and clinical development status for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Biology

Background:

  • Aurora A and B kinases are crucial regulators of cell division.
  • Dysregulation of these kinases is implicated in various cancers.
  • Targeting Aurora kinases presents a viable strategy for cancer treatment.

Purpose of the Study:

  • To review the rationale for targeting Aurora kinases in cancer.
  • To examine existing Aurora kinase inhibitors in scientific and patent literature.
  • To discuss inhibitor-target interactions, resistance mechanisms, and clinical development.

Main Methods:

  • Literature review of scientific and patent databases.
  • Analysis of published crystal structures of Aurora kinases.
  • Evaluation of preclinical and clinical data for Aurora kinase inhibitors.

Main Results:

  • Multiple Aurora kinase inhibitors have been identified and characterized.
  • Crystal structures reveal key binding interactions and potential resistance mutations.
  • Several inhibitors are progressing through clinical trials for cancer treatment.

Conclusions:

  • Aurora kinases remain attractive targets for cancer drug development.
  • Understanding kinase structure and resistance is vital for effective inhibitor design.
  • Clinical evaluation of Aurora kinase inhibitors is ongoing with promising potential.

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