Related Experiment Video

Updated: Jul 8, 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

Specific small-molecule activator of Aurora kinase A induces autophosphorylation in a cell-free system

A Hari Kishore1, B M Vedamurthy, K Mantelingu

  • 1Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 06, India.

Journal of Medicinal Chemistry
|January 25, 2008
PubMed

Insights

Anacardic acid from cashew nuts activates Aurora kinase A, a protein linked to cancer. This discovery offers a new tool for studying cancer-related genomic instability.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • Aurora kinases are crucial for cell division and genomic stability.
  • Aurora kinase A (AAK) is overexpressed in many cancers, but its role in tumorigenesis is unclear.

Purpose of the Study:

  • To identify small molecules that modulate Aurora kinase activity.
  • To investigate the potential of anacardic acid as a modulator of Aurora kinase A.

Main Methods:

  • Virtual screening was used to identify potential Aurora kinase inhibitors.
  • In vitro assays were performed to assess the effect of anacardic acid on Aurora kinase A and B activity.
  • Histone H3 phosphorylation was measured to evaluate Aurora kinase A activity.

Main Results:

  • Anacardic acid, derived from cashew nut shell liquid, was found to bind to Aurora kinases A and B.
  • Anacardic acid potently activated Aurora kinase A-mediated histone H3 phosphorylation in vitro.
  • Aurora kinase B activity remained unaffected at similar concentrations.
  • Anacardic acid induced structural changes and autophosphorylation of Aurora kinase A, enhancing its enzymatic activity.

Conclusions:

  • Anacardic acid is the first identified small-molecule activator of Aurora kinase A.
  • This compound can be a valuable tool for investigating the function of overexpressed Aurora kinase A in cancer.

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