Aurora-A Kinase as a Promising Therapeutic Target in Cancer

Frontiers in Oncology
Antonino B D'AssoroEvanthia Galanis

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.

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Citations

Aug 6, 2016·Frontiers in Genetics·Stefano Ferrari, Christian Gentili
Dec 26, 2016·Journal of Pathology and Translational Medicine·Hyun Min KohYoung Hee Maeng
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May 22, 2021·European Journal of Medicinal Chemistry·Tathagata PradhanVikramdeep Monga

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Methods Mentioned

BETA
xenografts

Clinical Trials Mentioned

NCT02038647
NCT01482962
NCT02219789
NCT02134067
NCT02448589

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