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

Abstract Aurora kinase A (AURKA) belongs to the family of serine/threonine kinases, whose activation is necessary for cell division processes via regulation of mitosis. AURKA shows significantly higher expression in cancer tissues than in normal control tissues for multiple tumor types according to...

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Main Authors: Ruijuan Du, Chuntian Huang, Kangdong Liu, Xiang Li, Zigang Dong
Format: Article
Language:English
Published: BMC 2021-01-01
Series:Molecular Cancer
Subjects:
Online Access:https://doi.org/10.1186/s12943-020-01305-3
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author Ruijuan Du
Chuntian Huang
Kangdong Liu
Xiang Li
Zigang Dong
author_facet Ruijuan Du
Chuntian Huang
Kangdong Liu
Xiang Li
Zigang Dong
author_sort Ruijuan Du
collection DOAJ
description Abstract Aurora kinase A (AURKA) belongs to the family of serine/threonine kinases, whose activation is necessary for cell division processes via regulation of mitosis. AURKA shows significantly higher expression in cancer tissues than in normal control tissues for multiple tumor types according to the TCGA database. Activation of AURKA has been demonstrated to play an important role in a wide range of cancers, and numerous AURKA substrates have been identified. AURKA-mediated phosphorylation can regulate the functions of AURKA substrates, some of which are mitosis regulators, tumor suppressors or oncogenes. In addition, enrichment of AURKA-interacting proteins with KEGG pathway and GO analysis have demonstrated that these proteins are involved in classic oncogenic pathways. All of this evidence favors the idea of AURKA as a target for cancer therapy, and some small molecules targeting AURKA have been discovered. These AURKA inhibitors (AKIs) have been tested in preclinical studies, and some of them have been subjected to clinical trials as monotherapies or in combination with classic chemotherapy or other targeted therapies.
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spelling doaj.art-a33cbc49f042464d85d4d0c3ee1412712022-12-21T22:02:30ZengBMCMolecular Cancer1476-45982021-01-0120112710.1186/s12943-020-01305-3Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapyRuijuan Du0Chuntian Huang1Kangdong Liu2Xiang Li3Zigang Dong4Department of Pathophysiology, School of Basic Medical Sciences, Zhengzhou UniversityDepartment of Pathophysiology, School of Basic Medical Sciences, Zhengzhou UniversityDepartment of Pathophysiology, School of Basic Medical Sciences, Zhengzhou UniversityDepartment of Pathophysiology, School of Basic Medical Sciences, Zhengzhou UniversityDepartment of Pathophysiology, School of Basic Medical Sciences, Zhengzhou UniversityAbstract Aurora kinase A (AURKA) belongs to the family of serine/threonine kinases, whose activation is necessary for cell division processes via regulation of mitosis. AURKA shows significantly higher expression in cancer tissues than in normal control tissues for multiple tumor types according to the TCGA database. Activation of AURKA has been demonstrated to play an important role in a wide range of cancers, and numerous AURKA substrates have been identified. AURKA-mediated phosphorylation can regulate the functions of AURKA substrates, some of which are mitosis regulators, tumor suppressors or oncogenes. In addition, enrichment of AURKA-interacting proteins with KEGG pathway and GO analysis have demonstrated that these proteins are involved in classic oncogenic pathways. All of this evidence favors the idea of AURKA as a target for cancer therapy, and some small molecules targeting AURKA have been discovered. These AURKA inhibitors (AKIs) have been tested in preclinical studies, and some of them have been subjected to clinical trials as monotherapies or in combination with classic chemotherapy or other targeted therapies.https://doi.org/10.1186/s12943-020-01305-3Aurora kinase aCancerRegulatorsSubstratesInhibitorsCombination therapy
spellingShingle Ruijuan Du
Chuntian Huang
Kangdong Liu
Xiang Li
Zigang Dong
Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy
Molecular Cancer
Aurora kinase a
Cancer
Regulators
Substrates
Inhibitors
Combination therapy
title Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy
title_full Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy
title_fullStr Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy
title_full_unstemmed Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy
title_short Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy
title_sort targeting aurka in cancer molecular mechanisms and opportunities for cancer therapy
topic Aurora kinase a
Cancer
Regulators
Substrates
Inhibitors
Combination therapy
url https://doi.org/10.1186/s12943-020-01305-3
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