國家衛生研究院 NHRI:Item 3990099045/5012
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    題名: Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein
    作者: Tsai, TY;Yeh, TK;Chen, X;Hsu, T;Jao, YC;Huang, CH;Song, JS;Huang, YC;Chien, CH;Chiu, JH;Yen, SC;Tang, HK;Chao, YS;Jiaang, WT
    貢獻者: Division of Biotechnology and Pharmaceutical Research
    摘要: Fibroblast activation protein (FAP) belongs to the prolyl peptidase family. FAP inhibition is expected to become a new antitumor target. Most known FAP inhibitors often resemble the dipeptide cleavage products, with a boroproline at the P1 site; however, these inhibitors also inhibit DPP-IV, DPP-II, DPP8, and DPP9. Potent and selective FAP inhibitor is needed in evaluating that FAP as a therapeutic target. Therefore, it is important to develop selective FAP inhibitors for the use of target validation. To achieve this, optimization of the nonselective DPP-IV inhibitor 8 led to the discovery of a new class of substituted 4-carboxymethylpyroglutamic acid diamides as FAP inhibitors. SAR studies resulted in a number of FAP inhibitors having IC(50) of <100 nM with excellent selectivity over DPP-IV, DPP-II, DPP8, and DPP9 (IC(50) > 100 muM). Compounds 18a, 18b, and 19 are the only known potent and selective FAP inhibitors, which prompts us to further study the physiological role of FAP.
    日期: 2010-08
    關聯: Journal of Medicinal Chemistry. 2010 Aug;53(18):6572-6583.
    Link to: http://dx.doi.org/10.1021/jm1002556
    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:000281753700005
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77956717491
    顯示於類別:[趙宇生(2002-2013)] 期刊論文
    [葉燈光] 期刊論文
    [陳新(2002-2015)] 期刊論文
    [蔣維棠] 期刊論文

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