A practical review of proteasome pharmacology

TA Thibaudeau, DM Smith, Q Ma - Pharmacological reviews, 2019 - Elsevier
The ubiquitin proteasome system (UPS) degrades individual proteins in a highly regulated
fashion and is responsible for the degradation of misfolded, damaged, or unneeded cellular …

Targeting the ubiquitin-proteasome pathway to overcome anti-cancer drug resistance

S Narayanan, CY Cai, YG Assaraf, HQ Guo… - Drug Resistance …, 2020 - Elsevier
Drug resistance is a major obstacle in the field of pre-clinical and clinical therapeutics. The
development of novel technologies and targeted therapies have yielded new modalities to …

Positioning of proteasome inhibitors in therapy of solid malignancies

MSF Roeten, J Cloos, G Jansen - Cancer chemotherapy and …, 2018 - Springer
Targeting of the protein degradation pathway, in particular, the ubiquitin-proteasome system,
has emerged as an attractive novel cancer chemotherapeutic modality. Although …

Molecular basis of resistance to proteasome inhibitors in hematological malignancies

D Niewerth, G Jansen, YG Assaraf, S Zweegman… - Drug resistance …, 2015 - Elsevier
Over the past decade, the proteasome inhibitor bortezomib (Velcade) has not only gained a
cornerstone position in the treatment of hematological malignancies, particularly multiple …

Proteasome inhibitor-adapted myeloma cells are largely independent from proteasome activity and show complex proteomic changes, in particular in redox and …

GP Soriano, L Besse, N Li, M Kraus, A Besse… - Leukemia, 2016 - nature.com
Adaptive resistance of myeloma to proteasome inhibition represents a clinical challenge,
whose biology is poorly understood. Proteasome mutations were implicated as underlying …

The proteasome as a druggable target with multiple therapeutic potentialities: Cutting and non-cutting edges

GR Tundo, D Sbardella, AM Santoro, A Coletta… - Pharmacology & …, 2020 - Elsevier
Abstract Ubiquitin Proteasome System (UPS) is an adaptable and finely tuned system that
sustains proteostasis network under a large variety of physiopathological conditions. Its …

Next-generation proteasome inhibitors for cancer therapy

JE Park, Z Miller, Y Jun, W Lee, KB Kim - Translational Research, 2018 - Elsevier
Over 2 decades ago, the proteasome was considered a risky or even untenable therapeutic
target. Today, proteasome inhibitors are a mainstay in the treatment of multiple myeloma …

Spotlight on ixazomib: potential in the treatment of multiple myeloma

B Muz, RN Ghazarian, M Ou, MJ Luderer… - Drug design …, 2016 - Taylor & Francis
Despite the significant therapeutic advances achieved with proteasome inhibitors (PIs) such
as bortezomib and carfilzomib in prolonging the survival of patients with multiple myeloma …

Proteasome inhibitors as experimental therapeutics of autoimmune diseases

SE Verbrugge, RJ Scheper, WF Lems… - Arthritis research & …, 2015 - Springer
Current treatment strategies for rheumatoid arthritis (RA) consisting of disease-modifying
anti-rheumatic drugs or biological agents are not always effective, hence driving the demand …

Brain-Permeable Immunoproteasome-Targeting Macrocyclic Peptide Epoxyketones for Alzheimer's Disease

JE Park, CL Chaudhary, D Bhattarai… - Journal of medicinal …, 2024 - ACS Publications
Previously, we demonstrated that linear peptide epoxyketones targeting the
immunoproteasome (iP) could ameliorate cognitive deficits in mouse models of Alzheimer's …