Proteasome inhibitors in cancer therapy

EE Manasanch, RZ Orlowski - Nature reviews Clinical oncology, 2017 - nature.com
The ubiquitin proteasome pathway was discovered in the 1980s to be a central component
of the cellular protein-degradation machinery with essential functions in homeostasis, which …

Overview of proteasome inhibitor-based anti-cancer therapies: perspective on bortezomib and second generation proteasome inhibitors versus future generation …

Q Ping Dou, JA Zonder - Current cancer drug targets, 2014 - ingentaconnect.com
Over the past ten years, proteasome inhibition has emerged as an effective therapeutic
strategy for treating multiple myeloma (MM) and some lymphomas. In 2003, Bortezomib …

[HTML][HTML] Xbp1s-negative tumor B cells and pre-plasmablasts mediate therapeutic proteasome inhibitor resistance in multiple myeloma

C Leung-Hagesteijn, N Erdmann, G Cheung, JJ Keats… - Cancer cell, 2013 - cell.com
Proteasome inhibitor (PI) resistance mechanisms in multiple myeloma (MM) remain
controversial. We report the existence of a progenitor organization in primary MM that …

The emergence of drug resistance to targeted cancer therapies: Clinical evidence

AB Sarmento-Ribeiro, A Scorilas, AC Gonçalves… - Drug Resistance …, 2019 - Elsevier
For many decades classical anti-tumor therapies included chemotherapy, radiation and
surgery; however, in the last two decades, following the identification of the genomic drivers …

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 …

Spectrum and functional validation of PSMB5 mutations in multiple myeloma

S Barrio, T Stühmer, M Da-Viá, C Barrio-Garcia… - Leukemia, 2019 - nature.com
Despite an increasing number of approved therapies, multiple myeloma (MM) remains an
incurable disease and only a small number of patients achieve prolonged disease control …

Targeting the insulin-like growth factor-1 receptor to overcome bortezomib resistance in preclinical models of multiple myeloma

DJ Kuhn, Z Berkova, RJ Jones… - Blood, The Journal …, 2012 - ashpublications.org
Proteasome inhibition with bortezomib is a validated approach to the treatment of multiple
myeloma, but drug resistance often emerges and limits its utility in the retreatment setting. To …

Impaired bortezomib binding to mutant β5 subunit of the proteasome is the underlying basis for bortezomib resistance in leukemia cells

NE Franke, D Niewerth, YG Assaraf, J van Meerloo… - Leukemia, 2012 - nature.com
Proteasome inhibition is a novel treatment for several hematological malignancies.
However, resistance to the proteasome inhibitor bortezomib (BTZ, Velcade) is an emerging …

[HTML][HTML] The resistance mechanisms of proteasome inhibitor bortezomib

S Lü, J Wang - Biomarker research, 2013 - Springer
The proteasome inhibitor, bortezomib, a boronic dipeptide which reversibly inhibit the
chymotrypsin-like activity at the β5-subunit of proteasome (PSMB5), has marked efficacy …

[HTML][HTML] Revisiting proteasome inhibitors: molecular underpinnings of their development, mechanisms of resistance and strategies to overcome anti-cancer drug …

C Leonardo-Sousa, AN Carvalho, RA Guedes… - Molecules, 2022 - mdpi.com
Proteasome inhibitors have shown relevant clinical activity in several hematological
malignancies, namely in multiple myeloma and mantle cell lymphoma, improving patient …