國家衛生研究院 NHRI:Item 3990099045/14113
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    题名: Discovery of potential neuroprotective agents against paclitaxel-induced peripheral neuropathy
    作者: Chen, YF;Wu, CH;Chen, LH;Lee, HW;Lee, JC;Yeh, TK;Chang, JY;Chou, MC;Wu, HL;Lai, YP;Song, JS;Yeh, KC;Chen, CT;Lee, CJ;Shia, KS;Shen, MR
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Chemotherapy-induced neurotoxicity is a common adverse effect of cancer treatment. No medication has been shown to be effective in the prevention or treatment of chemotherapy-induced neurotoxicity. Using minoxidil as an initial template for structural modifications in conjunction with an in vitro neurite outgrowth assay, an image-based high-content screening platform, and mouse behavior models, an effective neuroprotective agent CN016 was discovered. Our results showed that CN016 could inhibit paclitaxel-induced inflammatory responses and infiltration of immune cells into sensory neurons significantly. Thus, the suppression of proinflammatory factors elucidates, in part, the mechanism of action of CN016 on alleviating paclitaxel-induced peripheral neuropathy. Based on excellent efficacy in improving behavioral functions, high safety profiles (MTD > 500 mg/kg), and a large therapeutic window (MTD/MED > 50) in mice, CN016 might have great potential to become a peripherally neuroprotective agent to prevent neurotoxicity caused by chemotherapeutics as typified by paclitaxel.
    日期: 2022-03-02
    關聯: Journal of Medicinal Chemistry. 2022 Mar 2;65(6):4767-4782.
    Link to: http://dx.doi.org/10.1021/acs.jmedchem.1c01912
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000790749000021
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85126092860
    显示于类别:[張俊彥] 期刊論文
    [夏克山] 期刊論文
    [李靜琪] 期刊論文
    [葉燈光] 期刊論文
    [陳炯東] 期刊論文

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