Oxathiazolones selectively inhibit the human immunoproteasome over the constitutive proteasome
H Fan, NG Angelo, JD Warren… - ACS Medicinal …, 2014 - ACS Publications
Selective inhibitors for the human immunoproteasome LMP7 (β5i) subunit over the
constitutive proteasome hold promise for the treatment of autoimmune and inflammatory
diseases and hematologic malignancies. Here we report that oxathiazolones inhibit the
immunoproteasome β5i with up to 4700-fold selectivity over the constitutive proteasome, are
cell permeable, and inhibit proteasomes inside cells.
constitutive proteasome hold promise for the treatment of autoimmune and inflammatory
diseases and hematologic malignancies. Here we report that oxathiazolones inhibit the
immunoproteasome β5i with up to 4700-fold selectivity over the constitutive proteasome, are
cell permeable, and inhibit proteasomes inside cells.
Selective inhibitors for the human immunoproteasome LMP7 (β5i) subunit over the constitutive proteasome hold promise for the treatment of autoimmune and inflammatory diseases and hematologic malignancies. Here we report that oxathiazolones inhibit the immunoproteasome β5i with up to 4700-fold selectivity over the constitutive proteasome, are cell permeable, and inhibit proteasomes inside cells.
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