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 …
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 …
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 …
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
We describe noncovalent, reversible asparagine ethylenediamine (AsnEDA) inhibitors of the
Plasmodium falciparum proteasome (Pf20S) β5 subunit that spare all active subunits of …
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 …
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 …
multiple B-cell malignancies. These agents have also been employed with success in the …
[HTML][HTML] Immunoproteasome function in normal and malignant hematopoiesis
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 …
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 …
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 …
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 …
essential role in intracellular protein turnover. They are present in eukaryotes, archaea, and …