The pan-proteasome inhibitor bortezomib has demonstrated clinical efficacy in off label trials in SLE patients. The benefits of this study were accompanied by a number of adverse events that arise from inhibition of the constitutive proteasome. It was postulated that an immunoproteasome-selective inhibitor could sustain clinical efficacy and mitigate the safety liabilities associated with pan-proteasome inhibition. Herein, we disclose our efforts to identify beta 5i selective inhibitors using a ligand-based approach and the effect of these inhibitors in immune cells.<br/>

Design and evaluation of immunoproteasome-selective inhibitors for the treatment of autoimmune diseases

256th National Meeting (2018)

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