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  • Synthesis and biochemical evaluation of warhead-decorated psoralens as (immuno)proteasome inhibitors [Elektronski vir]
    Shannon Schiffrer, Eva ...
    The immunoproteasome is a multicatalytic protease that is predominantly expressed in cells of hematopoietic origin. Its elevated expression has been associated with autoimmune diseases, various types ... of cancer, and inflammatory diseases. Selective inhibition of its catalytic activities is therefore a viable approach for the treatment of these diseases. However, the development of immunoproteasome-selective inhibitors with non-peptidic scaffolds remains a challenging task. We previously reported 7H-furo[3,2-g]chromen-7-one (psoralen)-based compounds with an oxathiazolone warhead as selective inhibitors of the chymotrypsin-like ([beta]5i) subunit of immunoproteasome. Here, we describe the influence of the electrophilic warhead variations at position 3 of the psoralen core on the inhibitory potencies. Despite mapping the chemical space with different warheads, all compounds showed decreased inhibition of the [beta]5i subunit of immunoproteasome in comparison to the parent oxathiazolone-based compound. Although suboptimal, these results provide crucial information about structure-activity relationships that will serve as guidance for the further design of (immuno)proteasome inhibitors.
    Source: Molecules [Elektronski vir]. - ISSN 1420-3049 (Vol. 26, iss. 2, 2021, str. 1-18)
    Type of material - e-article ; adult, serious
    Publish date - 2021
    Language - english
    COBISS.SI-ID - 46540803

    Link(s):

    https://www.mdpi.com/1420-3049/26/2/356

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    Repository of the University of Ljubljana – RUL
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