M3258 is a selective inhibitor of the immunoproteasome subunit LMP7 (β5i) delivering efficacy in multiple myeloma models

MP Sanderson, M Friese-Hamim… - Molecular cancer …, 2021 - AACR
Abstract Large multifunctional peptidase 7 (LMP7/β5i/PSMB8) is a proteolytic subunit of the
immunoproteasome, which is predominantly expressed in normal and malignant …

Recent insights how combined inhibition of immuno/proteasome subunits enables therapeutic efficacy

M Basler, M Groettrup - Genes & Immunity, 2020 - nature.com
The proteasome is a multicatalytic protease in the cytosol and nucleus of all eukaryotic cells
that controls numerous cellular processes through regulated protein degradation …

[HTML][HTML] Cellular responses to proteasome inhibition: molecular mechanisms and beyond

N Albornoz, H Bustamante, A Soza… - International Journal of …, 2019 - mdpi.com
Proteasome inhibitors have been actively tested as potential anticancer drugs and in the
treatment of inflammatory and autoimmune diseases. Unfortunately, cells adapt to survive in …

[HTML][HTML] The functional and mechanistic roles of immunoproteasome subunits in cancer

SC Tripathi, D Vedpathak, EJ Ostrin - Cells, 2021 - mdpi.com
Cell-mediated immunity is driven by antigenic peptide presentation on major
histocompatibility complex (MHC) molecules. Specialized proteasome complexes called …

Exploring the proteasome system: A novel concept of proteasome inhibition and regulation

X Wang, T Meul, S Meiners - Pharmacology & Therapeutics, 2020 - Elsevier
The proteasome is a well-identified therapeutic target for cancer treatment. It acts as the
main protein degradation system in the cell and degrades key mediators of cell growth …

Comprehensive structure–activity relationship studies of cepafungin enabled by biocatalytic C–H oxidations

A Amatuni, A Shuster, D Abegg, A Adibekian… - ACS Central …, 2023 - ACS Publications
The cepafungins are a class of highly potent and selective eukaryotic proteasome inhibitor
natural products with potential to treat refractory multiple myeloma and other cancers. The …

Research Strategies of Small Molecules as Chemotherapeutics to Overcome Multiple Myeloma Resistance

J Yang, YC Yu, ZX Wang, QQ Li, N Ding… - European Journal of …, 2024 - Elsevier
Multiple myeloma (MM), a cancer of plasma cells, is the second most common
hematological malignancy which is characterized by aberrant plasma cells infiltration in the …

[HTML][HTML] At the cutting edge against cancer: a perspective on immunoproteasome and immune checkpoints modulation as a potential therapeutic intervention

GR Tundo, D Sbardella, F Oddone, AA Kudriaeva… - Cancers, 2021 - mdpi.com
Simple Summary Immunoproteasome plays a key role in the generation of antigenic
peptides. Immune checkpoints therapy is a front-line treatment of advanced/metastatic …

[HTML][HTML] Modulation of cellular redox parameters for improving therapeutic responses in multiple myeloma

A Allegra, C Petrarca, M Di Gioacchino, M Casciaro… - Antioxidants, 2022 - mdpi.com
Raised oxidative stress and abnormal redox status are typical features of multiple myeloma
cells, and the identification of the intimate mechanisms that regulate the relationships …

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 …