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Please use this identifier to cite or link to this item:
http://ir.nhri.org.tw/handle/3990099045/7568
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| Title: | BPR000K, a novel Aurora kinase inhibitor |
| Authors: | Chao, YS;Hsu, JTA;Chen, CT;Yeh, TK;Pan, SL;Hsieh, HP |
| Contributors: | Institute of Biotechnology and Pharmaceutical Research |
| Abstract: | Aurora kinases A, B, and C, members of sereine/threonine kinase, are key mitotic regulators involved in maintaining the genomic integrity of daughter cells. Because over-expression of Aurora A and Aurora B is frequently associated with tumor genesis, these molecules have been targeted for cancer therapy. Here we describe the profile of BPR000K, a specific and potent small molecule inhibitor discovered by the Institutes of Biotechnology and Pharmaceutical Research, National Health Research Institutes, targeting the Aurora kinase.BPR000K showed potent in vitro Aurora kinase A inhibition (IC50: 41 nM) and caused 4N-DNA accumulation at low concentration (26 nM). Moreover, BPR000K exhibited anticancer activity against a broad spectrum of cancer cells (IC50: 10~500 nM against Colo205, TW039, HCT-116, MOLM-13 and MIA Paca-2). In HCT-116 xenograft model, BPR000K suppressed tumor growth up to 90% at 20 mg/kg twice a day for 10-day treatment by IV administration, and showed better antitumoral activity than the reference agent (VX-680 at 50 mg/kg). The body weight loss is less than 10% during the dosing period. BPR000K also exhibited significant tumor regression in vivo by IV administration at 50 mg/kg once a day for 10-day treatment in Colo205 and MIA Paca-2 xenograft models. BPR000K suppressed tumor growth up to 90% at 50 mg/kg twice a day for 10-day treatment by IV administration in pencreative cancer xenograft models. |
| Date: | 2013-04-07 |
| Relation: | Abstracts of Papers - American Chemical Society. 2013 Apr 7;245:Article number 300-MEDI. |
| Link to: | http://abstracts.acs.org/chem/245nm/program/view.php?pub_num=300&par=MEDI |
| Cited Times(WOS): | https://www.webofscience.com/wos/woscc/full-record/WOS:000324303602320 |
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