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  • 3,1-benzothiazines, 1,4-benzodioxines, 1,4-benzoxazines as inhibitors of matriptase-2 [Elektronski vir] : outcome of a focused screening approach
    Roydeva, Polya G. ...
    The liver enzyme matriptase-2 is a multi-domain, transmembrane serine protease with an extracellular, C-terminal catalytic domain. Synthetic low-molecular weight inhibitors of matriptase-2 have ... potential as therapeutics to treat iron overload syndromes, in particular in patients with %-thalassemia. A sub-library of 64 compounds was screened for matriptase-2 inhibition and several active compounds were identified. (S)-Ethyl 2-(benzyl(3-((4-carbamidoylphenoxy)methyl)-2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-2-oxoacetate ((S)-12) showed an IC50 value of less than 10 %M. Structure-activity relationships were discussed and proposals to design new matriptase-2 inhibitors were made.
    Vir: Pharmaceuticals [Elektronski vir]. - ISSN 1424-8247 (Vol. 9, issue. 1, 2016, 11 str.)
    Vrsta gradiva - e-članek ; neleposlovje za odrasle
    Leto - 2016
    Jezik - angleški
    COBISS.SI-ID - 4018289

    Povezava(-e):

    http://www.mdpi.com/1424-8247/9/1/2

    Prosti dostop


    Repozitorij Univerze v Ljubljani – RUL
    DOI

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