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Updated: Mar 27, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Aurora-A Kinase as a Promising Therapeutic Target in Cancer
Antonino B D'Assoro1, Tufia Haddad2, Evanthia Galanis3
1Department of Medical Oncology, Mayo Clinic College of Medicine, Rochester, MN, USA; Department of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine, Rochester, MN, USA.
Abstract:
Mammalian Aurora family of serine/threonine kinases are master regulators of mitotic progression and are frequently overexpressed in human cancers. Among the three members of the Aurora kinase family (Aurora-A, -B, and -C), Aurora-A and Aurora-B are expressed at detectable levels in somatic cells undergoing mitotic cell division. Aberrant Aurora-A kinase activity has been implicated in oncogenic transformation through the development of chromosomal instability and tumor cell heterogeneity. Recent studies also reveal a novel non-mitotic role of Aurora-A activity in promoting tumor progression through activation of epithelial-mesenchymal transition reprograming resulting in the genesis of tumor-initiating cells. Therefore, Aurora-A kinase represents an attractive target for cancer therapeutics, and the development of small molecule inhibitors of Aurora-A oncogenic activity may improve the clinical outcomes of cancer patients. In the present review, we will discuss mitotic and non-mitotic functions of Aurora-A activity in oncogenic transformation and tumor progression. We will also review the current clinical studies, evaluating small molecule inhibitors of Aurora-A activity and their efficacy in the management of cancer patients.
Insights
Aurora-A kinase is crucial for cell division and cancer growth. Inhibiting its activity may offer new cancer treatment strategies by targeting both mitotic and non-mitotic functions.
Area of Science:
- Molecular Biology
- Cancer Biology
- Biochemistry
Background:
- Mammalian Aurora kinases regulate cell division and are often overexpressed in cancers.
- Aurora-A kinase plays key roles in mitotic progression and chromosomal stability.
- Aberrant Aurora-A activity contributes to tumor heterogeneity and oncogenic transformation.
Purpose of the Study:
- To review the mitotic and non-mitotic functions of Aurora-A in cancer.
- To discuss the therapeutic potential of targeting Aurora-A in cancer treatment.
- To evaluate clinical studies on small molecule inhibitors of Aurora-A.
Main Methods:
- Literature review of scientific publications.
- Analysis of studies on Aurora-A kinase functions.
- Evaluation of clinical trial data for Aurora-A inhibitors.
Main Results:
- Aurora-A kinase is involved in both cell division and non-mitotic processes like epithelial-mesenchymal transition.
- Its aberrant activity promotes tumor initiation, progression, and heterogeneity.
- Small molecule inhibitors targeting Aurora-A show promise in cancer therapy.
Conclusions:
- Aurora-A kinase is a significant therapeutic target for various human cancers.
- Targeting both mitotic and non-mitotic roles of Aurora-A may enhance treatment efficacy.
- Further clinical evaluation of Aurora-A inhibitors is warranted for improved cancer patient outcomes.
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