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Inhibition of human purine nucleoside phosphorylase by tenofovir phosphate congeners

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    0351497 - ÚOCHB 2011 RIV CZ eng J - Journal Article
    Votruba, Ivan - Trýznová, Jana - Břehová, Petra - Tloušťová, Eva - Horská, Květoslava - Fanfrlík, Jindřich - Přenosil, Ondřej - Holý, Antonín
    Inhibition of human purine nucleoside phosphorylase by tenofovir phosphate congeners.
    Collection of Czechoslovak Chemical Communications. Roč. 75, č. 12 (2010), s. 1249-1257. ISSN 0010-0765
    R&D Projects: GA MŠMT 1M0508
    Institutional research plan: CEZ:AV0Z40550506
    Keywords : purine nucleoside phosphorylase * phosphates of acyclic nucleoside * phosphonates * tenofovir phosphate congeners
    Subject RIV: CC - Organic Chemistry
    Impact factor: 0.853, year: 2010

    The structure-activity study on the phosphates of phosphonomethoxypropyl derivatives of purine bases interacting with human purine nucleoside phosphorylase has shown that the most efficient inhibitors of the enzyme are (R)- and (S)-PMPGp with Ki - 1.9 x 10-8 mol.l-1and/or 2.2 x 10-8 mol.l-1. These results were confirmed by docking studies.
    Permanent Link: http://hdl.handle.net/11104/0191236

     
     
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