Document Report Card

ID: ALA3259678

Journal: ACS Med Chem Lett

Title: Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome.

Authors: Fan H, Angelo NG, Warren JD, Nathan CF, Lin G.

Abstract: 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.

CiteXplore: 24900849

DOI: 10.1021/ml400531d