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Proteasome Inhibitors: Harnessing Proteostasis to Combat Disease [PDF]
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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Biosynthesis of lactacystin as a proteasome inhibitor [PDF]
Lactacystin is an irreversible proteasome inhibitor isolated from Streptomyces lactacystinicus. Despite its importance for its biological activity, the biosynthesis of lactacystin remains unknown. In this study, we identified the lactacystin biosynthetic
Takeshi Tsunoda +6 more
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Downregulation of 26S proteasome catalytic activity promotes epithelial-mesenchymal transition. [PDF]
The epithelial-mesenchymal transition (EMT) endows carcinoma cells with phenotypic plasticity that can facilitate the formation of cancer stem cells (CSCs) and contribute to the metastatic cascade.
Banno, Asoka +15 more
core +11 more sources
Metformin Induces Resistance of Cancer Cells to the Proteasome Inhibitor Bortezomib
The anti-diabetic drug metformin is currently tested for the treatment of hematological and solid cancers. Proteasome inhibitors, e.g., Bortezomib, are approved for the treatment of multiple myeloma and mantle cell lymphoma but are also studied for lung ...
Camille Schlesser +3 more
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The ubiquitin/proteasome system controls the stability of Runx2 and JunB, proteins essential for differentiation of mesenchymal progenitor/stem cells (MPCs) to osteoblasts.
Hengwei Zhang +6 more
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Synergistic apoptosis induction in leukemic cells by the phosphatase inhibitor salubrinal and proteasome inhibitors. [PDF]
Cells adapt to endoplasmic reticulum (ER)-stress by arresting global protein synthesis while simultaneously activating specific transcription factors and their downstream targets.
Hannes C A Drexler
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Resensitising proteasome inhibitor-resistant myeloma with sphingosine kinase 2 inhibition
The introduction of the proteasome inhibitor bortezomib into treatment regimens for myeloma has led to substantial improvement in patient survival.
Melissa K. Bennett +12 more
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Microbial proteasomes as drug targets.
Proteasomes are compartmentalized, ATP-dependent, N-terminal nucleophile hydrolases that play essentials roles in intracellular protein turnover. They are present in all 3 kingdoms.
Hao Zhang, Gang Lin
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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
openaire +4 more sources
Histone deacetylase (HDAC) inhibitors and proteasome inhibitors have been approved by the FDA for the treatment of multiple myeloma and lymphoma, respectively, but have not achieved similar activity as single agents in solid tumors.
Jianling Bi +7 more
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