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Please use this identifier to cite or link to this item:
http://ir.nhri.org.tw/handle/3990099045/13301
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| Title: | BPR6K609: An Aurora kinase inhibitor targeting small cell lung cancer with MYC amplification |
| Authors: | Chi, YH;Chang, CP;Ke, YY;Lin, WH;Wang, WP;Tsai, CH;Chen, YT;Su, YJ;Hung, MC;Wu, ZW;Wu, MH;Yeh, TK;Chen, CP;Song, JS;Chen, CT;Shih, C |
| Contributors: | Institute of Biotechnology and Pharmaceutical Research |
| Abstract: | Small cell lung cancer (SCLC) accounts for approximately 15% of all lung cancers, leading to ~30,000 deaths each year in the United States. SCLC patients often present with metastasis at time of diagnosis, excluding surgery as a treatment option. While patients show high response rate to standard chemotherapy such as cisplatin/etoposide, they soon develop drug resistance and disease progression. Therefore, new therapeutic strategies are urgently needed for SCLC. BPR6K609S0 is a novel Aurora kinase inhibitor which has been designed to inhibit the kinase activity of Aurora A, and induces proteasome-mediated degradation of MYC. The BPR6K609S0 active molecule provokes cell apoptosis and inhibits proliferation of several SCLC cell lines with IC50 < 100 nM. Oral administration of BPR6K609 induces >60 % tumor regression in a NCI-H446 xenograft mouse model. In addition, BPR6K609 further reduces tumor progression in NCI-H446 xenograft mice pre-treated with LY3295668, an Aurora A-selective inhibitor which is currently under clinical investigation. These results support the clinical potential of BRP6K609S0 for the treatment of SCLC. |
| Date: | 2020-08 |
| Relation: | Cancer Research. 2020 Aug;80(16):1937. |
| Link to: | http://dx.doi.org/10.1158/1538-7445.Am2020-1937 |
| JIF/Ranking 2023: | http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0008-5472&DestApp=IC2JCR |
| Cited Times(WOS): | https://www.webofscience.com/wos/woscc/full-record/WOS:000590059304170 |
| Appears in Collections: | [石全(2014-2017)] 會議論文/會議摘要
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