國家衛生研究院 NHRI:Item 3990099045/1247
English  |  正體中文  |  简体中文  |  全文笔数/总笔数 : 12145/12927 (94%)
造访人次 : 854828      在线人数 : 850
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/3990099045/1247


    题名: Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors
    作者: Lu, IL;Lee, SJ;Tsu, H;Wu, SY;Kao, KH;Chien, CH;Chang, YY;Chen, YS;Cheng, JH;Chang, CN;Chen, TW;Chang, SP;Chen, X;Jiaang, WT
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: To find potent and selective inhibitors of dipeptidyl peptidase IV (DPP-IV), we synthesized a series of 2-cyanopyrrolidine with P2-site 4-substituted glutamic acid derivatives and tested their activities against DPP-IV, DPP8, and DPP-II. Analogues that incorporated a bulky substituent at the first carbon position of benzylamine or isoquinoline showed over 30-fold selectivity for DPP-IV over both DPP8 and DPP-II. From structure-activity relationship studies, we speculate that the S2 site of DPP8 might be similar to that of DPP-IV, while DPP-IV inhibitor with N-substituted glycine in the P2 site and/or with a moiety involving in hydrophobic interaction with the side chain of Phe357 might provide a better selectivity for DPP-IV over DPP8.
    关键词: Chemistry, Medicinal;Chemistry, Organic
    日期: 2005-07-01
    關聯: Bioorganic and Medicinal Chemistry Letters. 2005 Jul;15(13):3271-3275.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2005.04.051
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0960-894X&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000230062300020
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=20444390974
    显示于类别:[蔣維棠] 期刊論文
    [伍素瑩] 期刊論文
    [李秀珠] 期刊論文
    [陳新(2002-2015)] 期刊論文

    文件中的档案:

    档案 描述 大小格式浏览次数
    000230062300020.pdf322KbAdobe PDF721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