Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome. Academic Article uri icon

Overview

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.

publication date

  • February 3, 2014

Identity

PubMed Central ID

  • PMC4027612

Scopus Document Identifier

  • 84898052676

Digital Object Identifier (DOI)

  • 10.1021/ml400531d

PubMed ID

  • 24900849

Additional Document Info

volume

  • 5

issue

  • 4