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Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
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Targeting aurora kinases in cancer treatment

Kevin R Kelly1, Jeffrey Ecsedy, Devalingam Mahalingam

  • 1The Institute for Drug Development, CTRC at University of Texas Health Science Center, 14960 Omicron Drive, San Antonio, TX 78245, USA.

Current Drug Targets
|July 23, 2011
PubMed

Insights

Aurora kinases are crucial for cell division and cancer. Inhibiting these kinases shows therapeutic promise in early clinical trials for treating various malignancies.

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Oncology

Background:

  • Aurora kinases are serine/threonine kinases vital for cell division processes like chromosome segregation and cytokinesis.
  • Dysregulation of Aurora kinase activity is implicated in the development and progression of numerous cancers.
  • Targeting Aurora kinases represents a promising strategy for cancer therapy.

Purpose of the Study:

  • To review the fundamental roles of Aurora kinases in normal cell division.
  • To discuss the involvement of Aurora kinases in various malignancies.
  • To summarize recent preclinical and clinical findings on Aurora kinase inhibitors in cancer treatment.

Main Methods:

  • Literature review of preclinical studies on Aurora kinase inhibitors.
  • Analysis of early-phase clinical trial data for Aurora kinase inhibitors.
  • Synthesis of information on cellular effects and therapeutic efficacy of Aurora kinase inhibition.

Main Results:

  • Aurora kinase inhibition impacts multiple stages of mitosis, including chromosome alignment and segregation.
  • Small molecule inhibitors targeting Aurora kinases demonstrate therapeutic efficacy in early clinical studies.
  • New insights into the cellular mechanisms of Aurora kinase inhibition have emerged.

Conclusions:

  • Aurora kinases are essential regulators of mitosis and are frequently overexpressed in cancers.
  • Aurora kinase inhibitors are emerging as a viable therapeutic option for cancer treatment.
  • Further investigation into the mechanism of action and clinical application of Aurora kinase inhibitors is warranted.

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