Literature DB >> 24900849

Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome.

Hao Fan1, Nicholas G Angelo1, J David Warren1, Carl F Nathan1, Gang Lin1.   

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.

Entities:  

Keywords:  Immunoproteasome; autoimmune disease; constitutive proteasome; selective inhibitor

Year:  2014        PMID： 24900849      PMCID： PMC4027612          DOI： 10.1021/ml400531d

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  23 in total

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