國家衛生研究院 NHRI:Item 3990099045/5909
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    题名: Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): Is DPP8-selectivity an attainable goal?
    作者: Van Goethem, S;Matheeussen, V;Joossens, J;Lambeir, AM;Chen, X;De Meester, I;Haemers, A;Augustyns, K;Van der Veken, P
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: This work represents the first directed study to identify modification points in the topology of a representative DPP8/9-inhibitor, capable of rendering selectivity for DPP8 over DPP9. The availability of a DPP8-selective compound would be highly instrumental for studying and untwining the biological roles of DPP8 and DPP9 and for the disambiguation of biological effects of nonselective DPP-inhibitors that have mainly been ascribed to blocking of DPPIV's action. The cell-permeable DPP8/9-inhibitor 7 was selected as a lead and dissected into several substructures that were modified separately for evaluating their potential to contribute to selectivity. The obtained results, together with earlier work from our group, clearly narrow down the most probable DPP8-selectivity imparting modification points in DPP8/9 inhibitors to parts of space that are topologically equivalent to the piperazine ring system in 7. This information can be considered of high value for future design of compounds with maximal DPP8 selectivity.
    日期: 2011-08
    關聯: Journal of Medicinal Chemistry. 2011 Aug;54(16):5737-5746.
    Link to: http://dx.doi.org/10.1021/jm200383j
    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:000294077300009
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=80051862999
    显示于类别:[陳新(2002-2015)] 期刊論文

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