Oxathiazolones selectively inhibit the human immunoproteasome over the constitutive proteasome
H Fan, NG Angelo, JD Warren… - ACS Medicinal …, 2014 - ACS Publications
Selective inhibitors for the human immunoproteasome LMP7 (β5i) subunit over the
constitutive proteasome hold promise for the treatment of autoimmune and inflammatory …
constitutive proteasome hold promise for the treatment of autoimmune and inflammatory …
Co‐inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity
M Basler, MM Lindstrom, JJ LaStant, JM Bradshaw… - EMBO …, 2018 - embopress.org
Cells of hematopoietic origin express high levels of the immunoproteasome, a cytokine‐
inducible proteasome variant comprising the proteolytic subunits LMP2 (β1i), MECL‐1 (β2i) …
inducible proteasome variant comprising the proteolytic subunits LMP2 (β1i), MECL‐1 (β2i) …
Structure-based optimization and discovery of M3258, a specific inhibitor of the immunoproteasome subunit LMP7 (β5i)
M Klein, M Busch, M Friese-Hamim… - Journal of Medicinal …, 2021 - ACS Publications
Proteasomes are broadly expressed key components of the ubiquitin-dependent protein
degradation pathway containing catalytically active subunits (β1, β2, and β5). LMP7 (β5i) is …
degradation pathway containing catalytically active subunits (β1, β2, and β5). LMP7 (β5i) is …
Discovery of highly selective inhibitors of the immunoproteasome low molecular mass polypeptide 2 (LMP2) subunit
HWB Johnson, JL Anderl, EK Bradley… - ACS Medicinal …, 2017 - ACS Publications
Building upon the success of bortezomib (VELCADE) and carfilzomib (KYPROLIS), the
design of a next generation of inhibitors targeting specific subunits within the …
design of a next generation of inhibitors targeting specific subunits within the …
Amelioration of autoimmunity with an inhibitor selectively targeting all active centres of the immunoproteasome
Background and Purpose Multicatalytic endopeptidase complex‐like‐1 (β2i), low molecular
mass polypeptide (LMP) 2 (β1i) and LMP7 (β5i) are the proteolytically active subunits of the …
mass polypeptide (LMP) 2 (β1i) and LMP7 (β5i) are the proteolytically active subunits of the …
[PDF][PDF] LMP2-specific inhibitors: chemical genetic tools for proteasome biology
YKA Ho, P Bargagna-Mohan, M Wehenkel, R Mohan… - Chemistry & biology, 2007 - cell.com
The immunoproteasome, having been linked to neurodegenerative diseases and
hematological cancers, has been shown to play an important role in MHC class I antigen …
hematological cancers, has been shown to play an important role in MHC class I antigen …
Design and evaluation of highly selective human immunoproteasome inhibitors reveal a compensatory process that preserves immune cell viability
E Ladi, C Everett, CE Stivala, BE Daniels… - Journal of Medicinal …, 2019 - ACS Publications
The pan-proteasome inhibitor bortezomib demonstrated clinical efficacy in off-label trials of
Systemic Lupus Erythematosus. One potential mechanism of this clinical benefit is from the …
Systemic Lupus Erythematosus. One potential mechanism of this clinical benefit is from the …
New insights into the function of the immunoproteasome in immune and nonimmune cells
H Kimura, P Caturegli, M Takahashi… - Journal of immunology …, 2015 - Wiley Online Library
The immunoproteasome is a highly efficient proteolytic machinery derived from the
constitutive proteasome and is abundantly expressed in immune cells. The …
constitutive proteasome and is abundantly expressed in immune cells. The …
[PDF][PDF] The immunoproteasome: a novel drug target for autoimmune diseases
The immunoproteasome, a special class of the proteasome, is mainly expressed in cells of
haematopoietic origin. Additionally, during inflammation, the immunoproteasome is induced …
haematopoietic origin. Additionally, during inflammation, the immunoproteasome is induced …
The immunoproteasome in antigen processing and other immunological functions
M Basler, CJ Kirk, M Groettrup - Current opinion in immunology, 2013 - Elsevier
Treatment of cells with interferon-γ leads to the replacement of the constitutive catalytic
proteasome subunits β1, β2, and β5 by the inducible subunits LMP2 (β1i), MECL-1 (β2i) …
proteasome subunits β1, β2, and β5 by the inducible subunits LMP2 (β1i), MECL-1 (β2i) …