國家衛生研究院 NHRI:Item 3990099045/13301

NHRI > Institute of Biotechnology and Pharmaceutical Research > Chuan Shih(2014-2017) > Conference Papers/Meeting Abstract > Item 3990099045/13301

Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/13301

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:	[Chuan Shih(2014-2017)] Conference Papers/Meeting Abstract [Chiung-Tong Chen] Conference Papers/Meeting Abstract [Teng-Kuang Yeh] Conference Papers/Meeting Abstract [Ya-Hui Chi] Conference Papers/Meeting Abstract [Chun-Ping Chang] Conference Papers/Meeting Abstract

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