國家衛生研究院 NHRI:Item 3990099045/7181
English  |  正體中文  |  简体中文  |  全文笔数/总笔数 : 12145/12927 (94%)
造访人次 : 906108      在线人数 : 715
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/3990099045/7181


    题名: Aurora kinase inhibitors reveal mechanisms of HURP in nucleation of centrosomal and kinetochore microtubules
    作者: Wu, JM;Chen, CT;Coumar, MS;Lin, WH;Chen, ZJ;Hsu, JT;Peng, YH;Shiao, HY;Chu, CY;Wu, JS;Lin, CT;Chen, CP;Hsueh, CC;Chang, KY;Kao, LP;Huang, CY;Chao, YS;Wu, SY;Hsieh, HP;Chi, YH
    贡献者: Institute of Biotechnology and Pharmaceutical Research;Institute of Cellular and Systems Medicine
    摘要: The overexpression of Aurora kinases in multiple tumors makes these kinases appealing targets for the development of anticancer therapies. This study identified two small molecules with a furanopyrimidine core, IBPR001 and IBPR002, that target Aurora kinases and induce a DFG conformation change at the ATP site of Aurora A. Our results demonstrate the high potency of the IBPR compounds in reducing tumorigenesis in a colorectal cancer xenograft model in athymic nude mice. Human hepatoma up-regulated protein (HURP) is a substrate of Aurora kinase A, which plays a crucial role in the stabilization of kinetochore fibers. This study used the IBPR compounds as well as MLN8237, a proven Aurora A inhibitor, as chemical probes to investigate the molecular role of HURP in mitotic spindle formation. These compounds effectively eliminated HURP phosphorylation, thereby revealing the coexistence and continuous cycling of HURP between unphosphorylated and phosphorylated forms that are associated, respectively, with microtubules emanating from centrosomes and kinetochores. Furthermore, these compounds demonstrate a spatial hierarchical preference for HURP in the attachment of microtubules extending from the mother to the daughter centrosome. The finding of inequality in the centrosomal microtubules revealed by these small molecules provides a versatile tool for the discovery of new cell-division molecules for the development of antitumor drugs.
    日期: 2013-05
    關聯: Proceedings of the National Academy of Sciences of the United States of America. 2013 May;110(19):E1779-E1787.
    Link to: http://dx.doi.org/10.1073/pnas.1220523110
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0027-8424&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000319327700011
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84877317722
    显示于类别:[謝興邦] 期刊論文
    [伍素瑩] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [徐祖安] 期刊論文
    [陳炯東] 期刊論文
    [紀雅惠] 期刊論文

    文件中的档案:

    档案 描述 大小格式浏览次数
    PUB23610398.pdf2120KbAdobe PDF903检视/开启


    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