國家衛生研究院 NHRI:Item 3990099045/8503
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    题名: Function-oriented development of CXCR4 antagonists as selective human immunodeficiency virus (HIV)-1 entry inhibitors
    作者: Wu, CH;Wang, CJ;Chang, CP;Cheng, YC;Song, JS;Jan, JJ;Chou, MC;Ke, YY;Ma, J;Wong, YC;Hsieh, TC;Tien, YC;Gullen, EA;Lo, CF;Cheng, CY;Liu, YW;Sadani, AA;Tsai, CH;Hsieh, HP;Tsou, LK;Shia, KS
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Motivated by the pivotal role of CXCR4 as an HIV entry co-receptor, we herein report a de novo hit-to-lead effort on the identification of subnanomolar purine-based CXCR4 antagonists against HIV-1 infection. Compound 24, with an EC50 of 0.5 nM against HIV-1 entry into host cells and an IC50 of 16.4 nM for inhibition of radioligand stromal-derived factor-1alpha (SDF-1alpha) binding to CXCR4, was also found to be highly selective against closely related chemokine receptors. We rationalized that compound 24 complementarily interacted with the critical CXCR4 residues that are essential for binding to HIV-1 gp120 V3 loop and subsequent viral entry. Compound 24 showed a 130-fold increase in anti-HIV activity compared to that of the marketed CXCR4 antagonist, AMD3100 (Plerixafor), whereas both compounds exhibited similar potency in mobilization of CXCR4+/CD34+ stem cells at a high dose. Our study offers insight into the design of anti-HIV therapeutics devoid of major interference with SDF-1alpha function.
    日期: 2015-02
    關聯: Journal of Medicinal Chemistry. 2015 Feb;58(3):1452-1465.
    Link to: http://dx.doi.org/10.1021/jm501772w
    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:000349573800034
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84922779010
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