Site-Specific Proteasome Inhibitors [PDF]
Biomolecules, 2021 Proteasome is a multi-subunit protein degradation machine, which plays a key role in the maintenance of protein homeostasis and, through degradation of regulatory proteins, in the regulation of numerous cell functions. Proteasome inhibitors are essential
Alexei F. Kisselev
doaj +3 more sources
Factors determining the sensitivity to proteasome inhibitors of multiple myeloma cells [PDF]
Frontiers in PharmacologyMultiple myeloma is an incurable cancer that originates from antibody-producing plasma cells. It is characterized by an intrinsic ability to produce large amounts of immunoglobulin-like proteins.
Marta Pelon +3 more
doaj +2 more sources
Early recovery of proteasome activity in cells pulse-treated with proteasome inhibitors is independent of DDI2 [PDF]
eLifeRapid recovery of proteasome activity may contribute to intrinsic and acquired resistance to FDA-approved proteasome inhibitors. Previous studies have demonstrated that the expression of proteasome genes in cells treated with sub-lethal concentrations of
Ibtisam Ibtisam, Alexei F Kisselev
doaj +2 more sources
Proteasome Inhibitors against Glioblastoma—Overview of Molecular Mechanisms of Cytotoxicity, Progress in Clinical Trials, and Perspective for Use in Personalized Medicine [PDF]
Current Oncology, 2023 Proteasome inhibitors are moieties targeting the proteolytic activity of a proteasome, with demonstrated efficacy in certain hematological malignancies and candidate drugs in other types of cancer, including glioblastoma (GBM). They disturb the levels of
Agata Gozdz
doaj +2 more sources
New Scaffolds of Proteasome Inhibitors: Boosting Anticancer Potential by Exploiting the Synergy of In Silico and In Vitro Methodologies [PDF]
Pharmaceuticals, 2023 Cancer is a complex multifactorial disease whose pathophysiology involves multiple metabolic pathways, including the ubiquitin–proteasome system, for which several proteasome inhibitors have already been approved for clinical use. However, the resistance
Romina A. Guedes +12 more
doaj +2 more sources
Proteasome inhibitors in cancer therapy [PDF]
Nature Reviews Clinical Oncology, 2017 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 include preventing the accumulation of misfolded or deleterious proteins.
Elisabet E Manasanch +2 more
exaly +3 more sources
Protocol for analysis of intracellular conversion of artezomib molecules into new proteasome inhibitors in Plasmodium falciparum parasites [PDF]
STAR ProtocolsSummary: Artezomibs (ATZs), dual-pharmacophore molecules comprising of artemisinin and a parasite proteasome inhibitor, hijack parasite ubiquitin proteasome system to transform into new proteasome inhibitors following the activation of artemisinin by ...
Wenhu Zhan +3 more
doaj +2 more sources
FoxM1 is a general target for proteasome inhibitors. [PDF]
PLoS ONE, 2009 Proteasome inhibitors are currently in the clinic or in clinical trials, but the mechanism of their anticancer activity is not completely understood. The oncogenic transcription factor FoxM1 is one of the most overexpressed genes in human tumors, while ...
Uppoor G Bhat +2 more
doaj +3 more sources
Proteasome inhibitors in cancer therapy [PDF]
Journal of Cell Communication and Signaling, 2011 The ubiquitin proteasome pathway plays a critical role in regulating many processes in the cell which are important for tumour cell growth and survival. Inhibition of proteasome function has emerged as a powerful strategy for anti-cancer therapy. Clinical validation of the proteasome as a therapeutic target was achieved with bortezomib and has prompted
Lisa J Crawford +2 more
exaly +4 more sources
The Role of Proteasome Inhibitors in Treating Acute Lymphoblastic Leukaemia
Frontiers in Oncology, 2021 Acute lymphoblastic leukaemia (ALL) is an aggressive haematolymphoid malignancy. The prognosis of ALL is excellent in paediatric population, however the outcome of relapse/refractory disease is dismal.
Chun-fung Sin, Pui-hei Marcus Man
doaj +1 more source