Drug development targeting the ubiquitin–proteasome system (UPS) for the treatment of human cancers

X Zhang, S Linder, M Bazzaro - Cancers, 2020 - mdpi.com
Cancer cells are characterized by a higher rate of protein turnover and greater demand for
protein homeostasis compared to normal cells. In this scenario, the ubiquitin–proteasome …

Novel proteasome inhibitors to overcome bortezomib resistance

AM Ruschak, M Slassi, LE Kay… - Journal of the National …, 2011 - academic.oup.com
The proteasome is an intracellular enzyme complex that degrades ubiquitin-tagged proteins
and thereby regulates protein levels within the cell. Given this important role in maintaining …

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 …

Mechanisms of proteasome inhibitor action and resistance in cancer

DJ McConkey, K Zhu - Drug Resistance Updates, 2008 - Elsevier
Proteasome inhibitors (PIs), such as bortezomib, carfilzomib or NPI-0052, have excellent
clinical activity in patients with multiple myeloma and mantle cell lymphoma, and they are …

Proteasomes and several aspects of their heterogeneity relevant to cancer

AV Morozov, VL Karpov - Frontiers in Oncology, 2019 - frontiersin.org
The life of every organism is dependent on the fine-tuned mechanisms of protein synthesis
and breakdown. The degradation of most intracellular proteins is performed by the ubiquitin …

The proteasome load versus capacity balance determines apoptotic sensitivity of multiple myeloma cells to proteasome inhibition

G Bianchi, L Oliva, P Cascio, N Pengo… - Blood, The Journal …, 2009 - ashpublications.org
Proteasome inhibitors (PIs) are effective against multiple myeloma (MM), but the
mechanisms of action and bases of individual susceptibility remain unclear. Recent work …

Targeting the proteasome: partial inhibition of the proteasome by bortezomib or deletion of the immunosubunit LMP7 attenuates experimental colitis

N Schmidt, E Gonzalez, A Visekruna, AA Kühl… - Gut, 2010 - gut.bmj.com
Background and aims Inflammatory bowel disease (IBD), comprising Crohn´ s disease and
ulcerative colitis, is characterised by chronic relapsing inflammation of the gut. Increased …

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 …

Mammalian proteasome subtypes: Their diversity in structure and function

B Dahlmann - Archives of biochemistry and biophysics, 2016 - Elsevier
The 20S proteasome is a multicatalytic proteinase catalysing the degradation of the majority
of intracellular proteins. Thereby it is involved in almost all basic cellular processes, which is …

Identification and targeting of mutant peptide neoantigens in cancer immunotherapy

DJ Verdon, MR Jenkins - Cancers, 2021 - mdpi.com
Simple Summary Cancerous cells acquire genetic mutations that can lead to changes in the
amino acid sequence of proteins. These altered amino acid sequences, or “neoantigens” …