LMP2-Specific Inhibitors: Chemical Genetic Tools for Proteasome Biology Article

Ho, YK, Bargagna-Mohan, P, Wehenkel, M et al. (2007). LMP2-Specific Inhibitors: Chemical Genetic Tools for Proteasome Biology . Chemistry and Biology, 14(4), 419-430. 10.1016/j.chembiol.2007.03.008

cited authors

  • Ho, YK; Bargagna-Mohan, P; Wehenkel, M; Mohan, R; Kim, KB

abstract

  • The immunoproteasome, having been linked to neurodegenerative diseases and hematological cancers, has been shown to play an important role in MHC class I antigen presentation. However, its other pathophysiological functions are still not very well understood. This can be attributed mainly to a lack of appropriate molecular probes that can selectively modulate the immunoproteasome catalytic subunits. Herein, we report the development of molecular probes that selectively inhibit the major catalytic subunit, LMP2, of the immunoproteasome. We show that these compounds irreversibly modify the LMP2 subunit with high specificity. Importantly, LMP2-rich cancer cells compared to LMP2-deficient cancer cells are more sensitive to growth inhibition by the LMP2-specific inhibitor, implicating an important role of LMP2 in regulating cell growth of malignant tumors that highly express LMP2. © 2007 Elsevier Ltd. All rights reserved.

authors

publication date

  • April 20, 2007

published in

Digital Object Identifier (DOI)

start page

  • 419

end page

  • 430

volume

  • 14

issue

  • 4