Molecular basis of the selectivity of the immunoproteasome catalytic subunit LMP2-specific inhibitor revealed by molecular modeling and dynamics simulations

B Lei, MDM Abdul Hameed, A Hamza… - The journal of …, 2010 - ACS Publications
Given that immunoproteasome inhibitors are currently being developed for a variety of
potent therapeutic purposes, the unique specificity of an α′, β′-epoxyketone peptide …

Immunoproteasomes: structure, function, and antigen presentation

DA Ferrington, DS Gregerson - Progress in molecular biology and …, 2012 - Elsevier
Immunoproteasomes contain replacements for the three catalytic subunits of standard
proteasomes. In most cells, oxidative stress and proinflammatory cytokines are stimuli that …

On the role of the immunoproteasome in transplant rejection

M Basler, J Li, M Groettrup - Immunogenetics, 2019 - Springer
The immunoproteasome is expressed in cells of hematopoietic origin and is induced during
inflammation by IFN-γ. Targeting the immunoproteasome with selective inhibitors has been …

Novel propeptide function in 20 S proteasome assembly influences β subunit composition

DJ Kingsbury, TA Griffin, RA Colbert - Journal of Biological Chemistry, 2000 - ASBMB
The assembly of eukaryotic 20 S proteasomes involves the formation of half-proteasomes
where precursor β-type subunits gather in position on an α-subunit ring, followed by the …

Structural plasticity of the proteasome and its function in antigen processing

M Groettrup, M van den Broek… - Critical Reviews™ in …, 2001 - dl.begellhouse.com
The proteasome is the main provider of peptide ligands for major histocompatibility complex
class I molecules. During an immune response to pathogens, the proinflammatory cytokine …

Selective inhibition of the immunoproteasome by ligand‐induced crosslinking of the active site

C Dubiella, H Cui, M Gersch… - Angewandte Chemie …, 2014 - Wiley Online Library
The concept of proteasome inhibition ranks among the latest achievements in the treatment
of blood cancer and represents a promising strategy for modulating autoimmune diseases …

Why the structure but not the activity of the immunoproteasome subunit low molecular mass polypeptide 2 rescues antigen presentation

M Basler, C Lauer, J Moebius, R Weber… - The Journal of …, 2012 - journals.aai.org
The proteasome is responsible for the generation of most epitopes presented on MHC class
I molecules. Treatment of cells with IFN-γ leads to the replacement of the constitutive …

Development of proteasome inhibitors in oncology and autoimmune diseases.

MK Bennett, CJ Kirk - Current opinion in drug discovery & …, 2008 - europepmc.org
The proteasome is a multicatalytic protease complex that mediates the controlled
degradation of intracellular proteins, including key components of pathways that contribute …

Structural elucidation of a nonpeptidic inhibitor specific for the human immunoproteasome

H Cui, R Baur, C Le Chapelain, C Dubiella… - …, 2017 - Wiley Online Library
Selective inhibition of the immunoproteasome is a promising approach towards the
development of immunomodulatory drugs. Recently, a class of substituted thiazole …

Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S β5-subunit

C Blackburn, KM Gigstad, P Hales, K Garcia… - Biochemical …, 2010 - portlandpress.com
The mammalian 26S proteasome is a 2500 kDa multi-catalytic complex involved in
intracellular protein degradation. We describe the synthesis and properties of a novel series …