國家衛生研究院 NHRI:Item 3990099045/15569
English  |  正體中文  |  简体中文  |  全文笔数/总笔数 : 12145/12927 (94%)
造访人次 : 906612      在线人数 : 972
RC Version 6.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
搜寻范围 查询小技巧：
  • 您可在西文检索词汇前后加上"双引号"，以获取较精准的检索结果
  • 若欲以作者姓名搜寻，建议至进阶搜寻限定作者字段，可获得较完整数据
    •  进阶搜寻
    主页 ‧ 登入 ‧ 上传 ‧ 说明 ‧ 关于NHRI ‧ 管理 到手机版


    jsp.display-item.identifier=請使用永久網址來引用或連結此文件: http://ir.nhri.org.tw/handle/3990099045/15569


    题名: Discovery of novel AXL and MER inhibitors as potential anticancer and immune modulator drugs
    作者: Hsieh, HP;Li, MC;Yen, WC;Hsu, JTA;Yeh, TK;Li, WS;Wu, HC
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Background: In cancer progression, abnormal expression of AXL could lead to tumor growth and metastasis and resistance to chemotherapy, while MER could identify apoptotic cancer cells and induce immune suppression in the tumor microenvironment. Combination of AXL and MER inhibitors could generate a synergistic effect, enhancing antitumor responses, and further suppressing resistance formed by monotherapy with AXL selective or MER selective inhibitors. According to the explicit function of AXL and MER, the….Methods: Based on our experience in the discovery of an anti-EGFR and anti-HER2 clinical candidate, we introduced several AXL-active and MER-active pharmacophores into DBPR112. We also modified the scaffold and the solubilizing groups to improve the drug-like properties. We have constructed a comprehensive SAR study to discover promising AXL and MER inhibitors…..Results: Upon synthesizing about 200 compounds, we identified several potent dual AXL and MER inhibitors. These compounds were evaluated for their anti-AXL and anti-MER activities, as well as their anti-tumor abilities. Our candidate 5K230 exhibited satisfied oral bioavailability (F% = 55%) and promising in vivo antitumor effects in several mouse xenograft models, including MDA-MB-231, 4T1, MC-38 tumors. Our compound also overcome erlotinib-acquired resistance via the combination with erlotinib in the..Conclusions: We have described the discovery of potential AXL and MER inhibitors, in which we identified potential candidate 5K230 which showed potent anti-AXL and anti-MER activities. Moreover, 5K230 displayed anti-tumor efficacy in several mouse xenograft models. Further preclinical evaluation of 5K230 is underway to develop it as a promising anticancer and immune modulator drug…
    日期: 2023-10
    關聯: Annals of Oncology. 2023 Oct;34(Suppl. 2):S214.
    Link to: http://dx.doi.org/10.1016/j.annonc.2023.09.1591
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0923-7534&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:001087480200089
    显示于类别:[謝興邦] 會議論文/會議摘要
    [顏婉菁] 會議論文/會議摘要
    [徐祖安] 會議論文/會議摘要
    [葉燈光] 會議論文/會議摘要

    文件中的档案:

    没有与此文件相关的档案.



    在NHRI中所有的数据项都受到原著作权保护.

    TAIR相关文章

    DSpace Software Copyright © 2002-2004  MIT &  Hewlett-Packard  /   Enhanced by   NTU Library IR team Copyright ©   - 回馈