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Updated: Jun 15, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Biology of Aurora A kinase: implications in cancer manifestation and therapy
Dhanasekaran Karthigeyan1, Sallekoppal B Benaka Prasad, Jayasha Shandilya
1Transcription and Disease Laboratory, Molecular Biology and Genetics Unit, Jawaharlal Nehru Centre for Advanced Scientific Research, Jakkur, Bangalore, India.
Abstract:
The Aurora A kinase belongs to serine/threonine group of kinases, well known for its role in cell cycle, especially in the regulation of mitosis. Numerous substrates of Aurora A kinase have been identified, which are predominantly related to cell cycle progression while some of them are transcription factors. Aurora A-mediated phosphorylation can either directly or indirectly regulate the function of its substrates. There are overwhelming evidences which report overexpression and gene amplification of Aurora A in several human cancers, and suggest that Aurora A could be a bona fide oncogene involved in tumorigenesis. Hence, Aurora A plays wide-ranging roles in both mitosis and its deregulation manifests in cancer progression. These observations have favored the choice of Aurora kinases as a target for cancer therapy. Recently, numerous small molecules have been discovered against Aurora kinases and many have entered clinical trials. Most of these small-molecule modulators designed are specific against either Aurora A or Aurora B, but some are dual inhibitors targeting the ATP-binding site which is highly conserved among the three human homologues of Aurora kinase. In this review, we discuss the physiological functions of Aurora A, interactions between Aurora A kinase and its cellular substrates, tumorigenesis mediated by Aurora A kinase upon overexpression, and small-molecule modulators of Aurora kinase as targets for cancer therapy.
Insights
Aurora A kinase regulates mitosis and cell cycle progression. Its overexpression drives tumorigenesis, making Aurora A a promising target for novel cancer therapies and small-molecule inhibitors.
Area of Science:
- Molecular Biology
- Cell Biology
- Oncology
Background:
- Aurora A kinase is a serine/threonine kinase crucial for cell cycle regulation, particularly mitosis.
- Overexpression and gene amplification of Aurora A are implicated in human tumorigenesis, suggesting its role as an oncogene.
- Aurora A kinase interacts with numerous substrates, influencing cell cycle progression and transcription.
Purpose of the Study:
- To review the physiological functions of Aurora A kinase.
- To explore the interactions between Aurora A kinase and its substrates.
- To discuss the role of Aurora A kinase in tumorigenesis and its potential as a cancer therapeutic target.
Main Methods:
- Literature review of studies on Aurora A kinase.
- Analysis of research on Aurora A kinase substrates and phosphorylation.
- Examination of evidence linking Aurora A kinase to cancer development.
- Overview of small-molecule inhibitors targeting Aurora kinases.
Main Results:
- Aurora A kinase plays critical roles in mitosis and cell cycle control.
- Deregulation of Aurora A kinase activity contributes to cancer progression.
- Numerous small-molecule inhibitors targeting Aurora kinases have been developed and entered clinical trials.
- Inhibitors can be specific for Aurora A or Aurora B, or dual inhibitors targeting conserved ATP-binding sites.
Conclusions:
- Aurora A kinase is a key regulator of mitosis and a significant factor in cancer development.
- Targeting Aurora A kinase with small-molecule inhibitors represents a promising strategy for cancer therapy.
- Further research into Aurora kinase inhibitors may lead to more effective cancer treatments.
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