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
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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
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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
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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
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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
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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
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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
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Proteasome Inhibitors: Harnessing Proteostasis to Combat Disease
Molecules, 2020 The proteasome is the central component of the main cellular protein degradation pathway. During the past four decades, the critical function of the proteasome in numerous physiological processes has been revealed, and proteasome activity has been linked
David J. Sherman, Jing Li
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Biomolecules, 2020 Currently, proteasome inhibitors bortezomib, carfilzomib, and ixazomib are successfully used in clinics to treat multiple myeloma. However, these agents show limited efficacy against solid tumors. Identification of drugs that can potentiate the action of
Janakiram R. Vangala +2 more
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Biochemical Pharmacology, 2015 Proteasome inhibitors have a 20 year history in cancer therapy. The first proteasome inhibitor, bortezomib (Velcade, PS-341), a break-through multiple myeloma treatment, moved rapidly through development from bench in 1994 to first approval in 2003. Bortezomib is a reversible boronic acid inhibitor of the chymotrypsin-like activity of the proteasome ...
Teicher, Beverly A. +1 more
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