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 …

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] Enhancing activity and overcoming chemoresistance in hematologic malignancies with bortezomib: preclinical mechanistic studies

N Reddy, MS Czuczman - Annals of oncology, 2010 - Elsevier
Background Proteasome inhibition results in antitumor activity through various mechanisms,
including disruption of cell cycle progression and control, induction of apoptosis, and …

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

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 …

[HTML][HTML] Advances in the understanding of mechanisms and therapeutic use of bortezomib

T Mujtaba, QP Dou - Discovery medicine, 2011 - ncbi.nlm.nih.gov
The ubiquitin-proteasome pathway regulates many basic cellular processes and has been
proven to be a promising target for cancer therapy. Bortezomib is the first US Food and Drug …

Bortezomib-resistant mutant proteasomes: structural and biochemical evaluation with carfilzomib and ONX 0914

EM Huber, W Heinemeyer, M Groll - Structure, 2015 - cell.com
Inhibition of the 20S proteasome by bortezomib (Velcade) constitutes a successfully applied
therapy for blood cancer. However, emerging resistance restricts its medicinal use. For …

Resistance to the proteasome inhibitors: Lessons from multiple myeloma and mantle cell lymphoma

M Gonzalez-Santamarta, G Quinet… - … and Disease: From …, 2020 - Springer
Since its introduction in the clinics in early 2000s, the proteasome inhibitor bortezomib (BTZ)
significantly improved the prognosis of patients with multiple myeloma (MM) and mantle cell …

Molecular mechanisms of bortezomib resistant adenocarcinoma cells

E Suzuki, S Demo, E Deu, J Keats, S Arastu-Kapur… - PloS one, 2011 - journals.plos.org
Bortezomib (Velcade™) is a reversible proteasome inhibitor that is approved for the
treatment of multiple myeloma (MM). Despite its demonstrated clinical success, some …

Proteasome inhibition as a new therapeutic principle in hematological malignancies

CS Mitsiades, N Mitsiades, T Hideshima… - Current drug …, 2006 - ingentaconnect.com
The intracellular concentration of proteins in both normal and tumor cells are regulated by
the balance between the rates of protein synthesis vs. degradation. The ubiquitin …

Molecular mechanisms of acquired proteasome inhibitor resistance

AJ Kale, BS Moore - Journal of medicinal chemistry, 2012 - ACS Publications
The development of proteasome inhibitors (PIs) has transformed the treatment of multiple
myeloma and mantle cell lymphoma. To date, two PIs have been FDA approved, the …