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 …

A nut for every bolt: subunit-selective inhibitors of the immunoproteasome and their therapeutic potential

EM Huber, M Groll - Cells, 2021 - mdpi.com
At the heart of the ubiquitin–proteasome system, the 20S proteasome core particle (CP)
breaks down the majority of intracellular proteins tagged for destruction. Thereby, the CP …

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 …

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 …

A dual inhibitor of the proteasome catalytic subunits LMP2 and Y attenuates disease progression in mouse models of Alzheimer's disease

IJ Yeo, MJ Lee, A Baek, Z Miller, D Bhattarai… - Scientific reports, 2019 - nature.com
The immunoproteasome (iP) is a variant of the constitutive proteasome (cP) that is
abundantly expressed in immune cells which can also be induced in somatic cells by …

LMP2 inhibitors as a potential treatment for Alzheimer's Disease

D Bhattarai, MJ Lee, A Baek, IJ Yeo… - Journal of Medicinal …, 2020 - ACS Publications
The immunoproteasome (iP), an inducible proteasome variant harboring three
immunosubunits, low molecular mass polypeptide-2 (LMP2), multicatalytic endopeptidase …

Targeting proteasomes in cancer and infectious disease: a parallel strategy to treat malignancies and microbes

JJ Ignatz-Hoover, EV Murphy… - Frontiers in Cellular and …, 2022 - frontiersin.org
Essential core pathways of cellular biology are preserved throughout evolution, highlighting
the importance of these pathways for both bacteria and human cancer cells alike. Cell …

Covalent small molecule immunomodulators targeting the protease active site

HR Kim, R Tagirasa, E Yoo - Journal of Medicinal Chemistry, 2021 - ACS Publications
Cells of the immune system utilize multiple proteases to regulate cell functions and
orchestrate innate and adaptive immune responses. Dysregulated protease activities are …

Structure-based design of inhibitors selective for human proteasome β2c or β2i subunits

BT Xin, EM Huber, G de Bruin… - Journal of medicinal …, 2019 - ACS Publications
Subunit-selective proteasome inhibitors are valuable tools to assess the biological and
medicinal relevance of individual proteasome active sites. Whereas the inhibitors for the …

Immunoproteasome-selective inhibitors: the future of autoimmune diseases?

C Zhang, H Zhu, J Shao, R He, J Xi… - Future Medicinal …, 2020 - Taylor & Francis
The immunoproteasome, a specialized variant of the constitutive one, is predominantly
expressed in lymphocytes and monocytes of jawed vertebrates and is considered to be …