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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 대한약리학회 The Korean Journal of Physiology & Pharmacology The Korean Journal of Physiology & Pharmacology 제23권 제5호
- 발행연도
- 2019.1
- 수록면
- 393 - 402 (10page)
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초록· 키워드
오류제보하기
Aurora kinases inhibitors, including ZM447439 (ZM), which suppress cell division, have attracted a great deal of attention as potential novel anti-cancer drugs. Several recent studies have confirmed the anti-cancer effects of ZM in various cancer cell lines. However, there have been no studies regarding the cardiac safety of this agent. We performed several cytotoxicity, invasion and migration assays to examine the anti-cancer effects of ZM. To evaluate the potential effects of ZM on cardiac repolarisation, whole-cell patch-clamp experiments were performed with human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) and cells with heterogeneous cardiac ion channel expression. We also conducted a contractility assay with rat ventricular myocytes to determine the effects of ZM on myocardial contraction and/or relaxation. In tests to determine in vitro efficacy, ZM inhibited the proliferation of A549, H1299 (lung cancer), MCF-7 (breast cancer) and HepG2 (hepatoma) cell lines with IC50 in the submicromolar range, and attenuated the invasive and metastatic capacity of A549 cells. In cardiac toxicity testing, ZM did not significantly affect I Na, I Ks or I K1, but decreased I hERG in a dose-dependent manner (IC50: 6.53 μM). In action potential (AP) assay using hiPSC-CMs, ZM did not induce any changes in AP parameters up to 3 μM, but it at 10 M induced prolongation of AP duration. In summary, ZM showed potent broad-spectrum anti-tumor activity, but relatively low levels of cardiac side effects compared to the effective doses to tumor. Therefore, ZM has a potential to be a candidate as an anti-cancer with low cardiac toxicity.
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참고문헌 (30)
참고문헌 신청
Cirak Y / 2015 / Aurora A overexpression in breast cancer patients induces taxane resistance and results in worse prognosis / J BUON 20:1414~1419
Zhang Y / 2015 / Elevated Aurora B expression contributes to chemoresistance and poor prognosis in breast cancer / Int J Clin Exp Pathol 8:751~757
Zekri A / 2012 / Gene amplification and overexpression of Aurora-C in breast and prostate cancer cell lines / Oncol Res 20:241~250
Yang H / 2004 / Aurora-A kinase regulates telomerase activity through c-Myc in human ovarian and breast epithelial cells / Cancer Res 64:463~467
Gavriilidis P / 2015 / Aurora kinases and potential medical applications of aurora kinase inhibitors : a review / J Clin Med Res 7:742~751
Zhang Y / 2015 / Elevated Aurora B expression contributes to chemoresistance and poor prognosis in breast cancer / Int J Clin Exp Pathol 8:751~757
Zekri A / 2012 / Gene amplification and overexpression of Aurora-C in breast and prostate cancer cell lines / Oncol Res 20:241~250
Yang H / 2004 / Aurora-A kinase regulates telomerase activity through c-Myc in human ovarian and breast epithelial cells / Cancer Res 64:463~467
Gavriilidis P / 2015 / Aurora kinases and potential medical applications of aurora kinase inhibitors : a review / J Clin Med Res 7:742~751
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