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Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy

Ruijuan Du1,2, Chuntian Huang3,4, Kangdong Liu3,4,5,6

  • 1Department of Pathophysiology, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450001, Henan, China. RJDu@hci-cn.org.

Molecular Cancer
|January 16, 2021
PubMed

Insights

Aurora kinase A (AURKA) is crucial for cell division and often overexpressed in cancers. Targeting AURKA with inhibitors shows promise for novel cancer therapies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cell Biology

Background:

  • Aurora kinase A (AURKA) is a serine/threonine kinase essential for cell division and mitosis.
  • AURKA exhibits elevated expression in various cancer types compared to normal tissues, as evidenced by TCGA data.
  • AURKA's role in cancer progression is supported by identified substrates involved in cell cycle regulation and oncogenesis.

Purpose of the Study:

  • To review the role of AURKA in cancer development and progression.
  • To explore the potential of AURKA as a therapeutic target in oncology.
  • To summarize the development and clinical evaluation of AURKA inhibitors (AKIs).

Main Methods:

  • Analysis of TCGA database for AURKA expression levels in different cancers.
  • Identification and functional analysis of AURKA substrates.
  • Review of preclinical and clinical studies on AURKA inhibitors.

Main Results:

  • AURKA overexpression is a common feature across multiple tumor types.
  • AURKA substrates include key regulators of mitosis, tumor suppressors, and oncogenes.
  • KEGG pathway and GO analysis reveal AURKA-interacting proteins are involved in oncogenic pathways.

Conclusions:

  • AURKA is a validated target for cancer therapy due to its critical role in cell division and oncogenesis.
  • Numerous small molecule AURKA inhibitors (AKIs) have been developed.
  • AKIs are under investigation in preclinical and clinical trials as monotherapies or in combination treatments.
Keywords:
Aurora kinase aCancerCombination therapyInhibitorsRegulatorsSubstrates

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