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Ref Type Journal Article
PMID (24899685)
Authors Zheng FM, Long ZJ, Hou ZJ, Luo Y, Xu LZ, Xia JL, Lai XJ, Liu JW, Wang X, Kamran M, Yan M, Shao SJ, Lam EW, Wang SW, Lu G, Liu Q
Title A novel small molecule aurora kinase inhibitor attenuates breast tumor-initiating cells and overcomes drug resistance.
Journal Vol Issue Date Pages Journal Short Title
Molecular cancer therapeutics 13 8 2014 Aug 1991-2003 Mol Cancer Ther
URL
Abstract Text Chemoresistance is a major cause of cancer treatment failure. Tumor-initiating cells (TIC) have attracted a considerable amount of attention due to their role in chemoresistance and tumor recurrence. Here, we evaluated the small molecule Aurora kinase inhibitor AKI603 as a novel agent against TICs in breast cancer. AKI603 significantly inhibited Aurora-A (AurA) kinase and induced cell-cycle arrest. In addition, the intragastric administration of AKI603 reduced xenograft tumor growth. Interestingly, we found that breast cancer cells that were resistant to epirubicin expressed a high level of activated AurA and also have a high CD24(Low)/CD44(High) TIC population. The inhibition of AurA kinase by AKI603 abolished the epirubicin-induced enrichment of TICs. Moreover, AKI603 suppressed the capacity of cells to form mammosphere and also suppressed the expression of self-renewal genes (β-catenin, c-Myc, Sox2, and Oct4). Thus, our work suggests the potential clinical use of the small molecule Aurora kinase inhibitor AKI603 to overcome drug resistance induced by conventional chemotherapeutics in breast cancer.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
AKI603 AKI603 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
AKI603 Aurka Inhibitors 26 AKI603 is a small molecule inhibitor of Aurora Kinase A, which may induce cell cycle arrest and inhibit cell proliferation and tumor growth (PMID: 24899685, PMID: 28592839).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References