title: Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome.
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.
authors.affiliation: Department of Microbiology & Immunology and Department of Biochemistry, Weill Cornell Medical College , 1300 York Avenue, New York, New York 10065, United States.
authors.forename: Hao
authors.initials: H
authors.lastname: Fan
authors.affiliation: Department of Microbiology & Immunology and Department of Biochemistry, Weill Cornell Medical College , 1300 York Avenue, New York, New York 10065, United States.
authors.forename: Nicholas G
authors.initials: NG
authors.lastname: Angelo
authors.affiliation: Department of Microbiology & Immunology and Department of Biochemistry, Weill Cornell Medical College , 1300 York Avenue, New York, New York 10065, United States.
authors.forename: J David
authors.initials: JD
authors.lastname: Warren
authors.affiliation: Department of Microbiology & Immunology and Department of Biochemistry, Weill Cornell Medical College , 1300 York Avenue, New York, New York 10065, United States.
authors.forename: Carl F
authors.initials: CF
authors.lastname: Nathan
authors.affiliation: Department of Microbiology & Immunology and Department of Biochemistry, Weill Cornell Medical College , 1300 York Avenue, New York, New York 10065, United States.
authors.forename: Gang
authors.initials: G
authors.lastname: Lin
keywords: Immunoproteasome; autoimmune disease; constitutive proteasome; selective inhibitor