國家衛生研究院 NHRI:Item 3990099045/1247
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    Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/1247


    Title: Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors
    Authors: 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
    Contributors: Division of Biotechnology and Pharmaceutical Research
    Abstract: 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.
    Keywords: Chemistry, Medicinal;Chemistry, Organic
    Date: 2005-07-01
    Relation: 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
    Appears in Collections:[Weir-Torn Jiaang] Periodical Articles
    [Su-Ying Wu] Periodical Articles
    [Shiow-Ju Lee] Periodical Articles
    [Xin Chen(2002-2015)] Periodical Articles

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