The proteasome in modern drug discovery: second life of a highly valuable drug target

PM Cromm, CM Crews - ACS central science, 2017 - ACS Publications
As the central figure of the cellular protein degradation machinery, the proteasome is critical
for cell survival. Having been extensively targeted for inhibition, the constitutive proteasome …

[HTML][HTML] Site-specific proteasome inhibitors

AF Kisselev - Biomolecules, 2021 - mdpi.com
Proteasome is a multi-subunit protein degradation machine, which plays a key role in the
maintenance of protein homeostasis and, through degradation of regulatory proteins, in the …

Immunoproteasome-selective and non-selective inhibitors: A promising approach for the treatment of multiple myeloma

R Ettari, M Zappalà, S Grasso, C Musolino… - Pharmacology & …, 2018 - Elsevier
The ubiquitin-proteasome system (UPS) is the major non-lysosomal proteolytic system for
the degradation of abnormal or damaged proteins no longer required. The proteasome is …

Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance

LA Kirkman, W Zhan, J Visone… - Proceedings of the …, 2018 - National Acad Sciences
We describe noncovalent, reversible asparagine ethylenediamine (AsnEDA) inhibitors of the
Plasmodium falciparum proteasome (Pf20S) β5 subunit that spare all active subunits of …

[HTML][HTML] Microbial proteasomes as drug targets

H Zhang, G Lin - PLoS Pathogens, 2021 - journals.plos.org
Proteasomes are compartmentalized, ATP-dependent, N-terminal nucleophile hydrolases
that play essentials roles in intracellular protein turnover. They are present in all 3 kingdoms …

[HTML][HTML] Discovery and early clinical development of selective immunoproteasome inhibitors

CJ Kirk, T Muchamuel, J Wang, RA Fan - Cells, 2021 - mdpi.com
Inhibitors of the proteolytic activity of the 20S proteasome have transformed the treatment of
multiple B-cell malignancies. These agents have also been employed with success in the …

[HTML][HTML] Immunoproteasome function in normal and malignant hematopoiesis

N Tubío-Santamaría, F Ebstein, FH Heidel, E Krüger - Cells, 2021 - mdpi.com
The ubiquitin–proteasome system (UPS) is a central part of protein homeostasis, degrading
not only misfolded or oxidized proteins but also proteins with essential functions. The fact …

Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases

J Xi, R Zhuang, L Kong, R He, H Zhu… - European Journal of …, 2019 - Elsevier
The immunoproteasome, a specialized form of proteasome, is mainly expressed in
lymphocytes and monocytes of jawed vertebrates and responsible for the generation of …

Subunit specific inhibitors of proteasomes and their potential for immunomodulation

AF Kisselev, M Groettrup - Current opinion in chemical biology, 2014 - Elsevier
Highlights•Structure–function relationship of subunit selective proteasome inhibitors.•
Development and characterization of new inhibitors of the immunoproteasome.•Modulation …

Targeting proteasomes in infectious organisms to combat disease

B Bibo‐Verdugo, Z Jiang, CR Caffrey… - The FEBS …, 2017 - Wiley Online Library
Proteasomes are multisubunit, energy‐dependent, proteolytic complexes that play an
essential role in intracellular protein turnover. They are present in eukaryotes, archaea, and …