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  • Nonpeptidic selective inhibitors of the chymotrypsin-like (ß5i) subunit of the immunoproteasome : Elektronski vir
    Sosič, Izidor ...
    Elevated expression of the immunoproteasome has been associated with autoimmune diseases, inflammatory diseases, and various types of cancer. Selective inhibitors of the immunoproteasome are not only ... scarce, but also almost entirely restricted to peptide-based compounds. Herein, we describe nonpeptidic reversible inhibitors that selectively block the chymotrypsin-like (ß5i) subunit of the human immunoproteasome in the low micromolar range. The most potent of the reversibly acting compounds were then converted into covalent, irreversible, nonpeptidic inhibitors that retained selectivity for the ß5i subunit. In addition, these inhibitors discriminate between the immunoproteasome and the constitutive proteasome in cell-based assays. Along with their lack of cytotoxicity, these data point to these nonpeptidic compounds being suitable for further investigation as ß5i-selective probes for possible application in noncancer diseases related to the immunoproteasome.
    Source: Angewandte Chemie : International edition. - ISSN 1433-7851 (Vol. 55, iss. 19, 2016, str. 5745-5748)
    Type of material - e-article ; adult, serious
    Publish date - 2016
    Language - english
    COBISS.SI-ID - 4050545

    Link(s):

    http://onlinelibrary.wiley.com/doi/10.1002/anie.201600190/abstract

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