Related Experiment Video

Updated: May 13, 2026

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

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

Published on: July 30, 2020

Aurora kinase targeted therapeutics in oncology: past, present and future

Daruka Mahadevan1, Sunni Beeck

  • 1Arizona Cancer Center, Tucson, AZ, 85724, USA +1 520 626 0191 ; +1 520 626 2255 ; dmahadevan@azcc.arizona.edu.

Expert Opinion on Drug Discovery
|March 15, 2013
PubMed

Insights

Aurora kinases (A, B, and C) are crucial for cell division and are overexpressed in cancers. Inhibitors targeting these kinases show promise for cancer treatment.

Area of Science:

  • Biochemistry
  • Cell Biology
  • Oncology

Background:

  • Aurora kinases (A, B, C) are serine-threonine kinases regulating mitosis.
  • Overexpression of Aurora kinases is linked to human cancers and polyploidy.
  • Small molecule inhibitors targeting Aurora kinases have been developed.

Purpose of the Study:

  • To investigate the role of Aurora kinases in cancer.
  • To explore the development of Aurora kinase inhibitors for cancer therapy.

Main Methods:

  • X-ray crystallography of Aurora kinases with inhibitors.
  • Fragment-based drug discovery.
  • Antitumor activity assessment in rodent cancer models.
  • Evaluation in Phase I clinical trials.

Main Results:

  • Crystal structures reveal inhibitor binding and resistance hotspots.
  • Specific inhibitors for Aurora A or B have been identified.
  • Aurora inhibitors demonstrate significant antitumor effects in preclinical models.

Conclusions:

  • Structural insights facilitate rational drug design for Aurora inhibitors.
  • Aurora inhibitors show therapeutic potential in various cancers.
  • Further clinical evaluation and combination strategies are warranted.

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