Targeting the Immunoproteasome in Health and Disease

S Mundt - 2016 - kops.uni-konstanz.de
The proteasome is a multicatalytic enzyme expressed in all eukaryotic cells and responsible
for the degradation of polyubiquitinated proteins. Thereby, the proteasome regulates protein …

[PDF][PDF] The immunoproteasome: a novel drug target for autoimmune diseases

M Basler, S Mundt, A Bitzer, C Schmidt… - Clin Exp …, 2015 - clinexprheumatol.org
The immunoproteasome, a special class of the proteasome, is mainly expressed in cells of
haematopoietic origin. Additionally, during inflammation, the immunoproteasome is induced …

[HTML][HTML] On the role of the immunoproteasome in protein homeostasis

M Basler, M Groettrup - Cells, 2021 - mdpi.com
Numerous cellular processes are controlled by the proteasome, a multicatalytic protease in
the cytosol and nucleus of all eukaryotic cells, through regulated protein degradation. The …

Immunoproteasome subunit LMP7 deficiency and inhibition suppresses Th1 and Th17 but enhances regulatory T cell differentiation

KW Kalim, M Basler, CJ Kirk… - The Journal of …, 2012 - journals.aai.org
The immunoproteasome generates peptides presented on MHC class I molecules to
cytotoxic T cells. ONX 0914 (formerly called PR-957) is a selective inhibitor of the …

Targeting the immunoproteasome and VCP/p97 in autoimmune disorders and viral infection

M del Río Oliva - 2022 - kops.uni-konstanz.de
The proteasome is a multicatalytic system involved in the degradation of polyubiquitinated
proteins. Thus, the proteasome is key to maintaining cell homeostasis. Stress and pro …

The immunoproteasome: an emerging therapeutic target

W Lee, K Bo Kim - Current topics in medicinal chemistry, 2011 - ingentaconnect.com
The proteasome, a large multisubunit protease complex, has been extensively investigated
over the years, greatly enhancing our understanding of critical roles that the proteasome …

Amelioration of autoimmunity with an inhibitor selectively targeting all active centres of the immunoproteasome

M Basler, E Maurits, G de Bruin… - British Journal of …, 2018 - Wiley Online Library
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 …

Abstract LB-054: Discovery and profiling of M3258, a potent and selective LMP7 inhibitor demonstrating high efficacy in multiple myeloma models

M Klein, M Busch, C Esdar, M Friese-Hamim, M Krier… - Cancer Research, 2019 - AACR
Proteasomes are large multi-subunit proteolytic complexes which are key components of the
ubiquitin-dependent protein degradation pathway. The constitutive proteasome is an isoform …

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 …

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) …