國家衛生研究院 NHRI:Item 3990099045/1231
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    題名: Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8
    作者: Jiaang, WT;Chen, YS;Hsu, T;Wu, SH;Chien, CH;Chang, CN;Chang, SP;Lee, SJ;Chen, X
    貢獻者: Division of Biotechnology and Pharmaceutical Research
    摘要: DPP8 is a prolyl dipeptidase homologous to DPP-IV, which is a drug target for Type 11 diabetes. The biological function of DPP8 is not known. To identify potent and selective chemical compounds against DPP8, we have synthesized a series of isoquinoline and isoindoline derivatives and have tested their inhibitory activity against DPP8, DPP-IV and DPP-II. Isoindoline derivatives were found to be more potent DPP8 inhibitors than isoquinoline derivatives. Isoindoline with a 1-(4,4'-difluor-benzhydryl)-piperazine group at the P2 site was observed to be a very potent DPP8 inhibitor, having an IC50 value of 14nM with at least a 2500-fold selectivity over either DPP-IV or DPP-II. From SAR results, we speculate that the S I site of DPP8 may be larger than that of DPPIV, which would allow the accommodation of larger C-terminal residues, such as isoquinoline or isoindoline.
    關鍵詞: Chemistry, Medicinal;Chemistry, Organic
    日期: 2005-02-01
    關聯: Bioorganic and Medicinal Chemistry Letters. 2005 Feb;15(3):687-691.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2004.11.023
    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:000226935700039
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=12444313913
    顯示於類別:[陳新(2002-2015)] 期刊論文
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    [蔣維棠] 期刊論文

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