Results 1 to 10 of about 223,575 (250)

Proteasome Inhibitors: Harnessing Proteostasis to Combat Disease [PDF]

open access: yesMolecules, 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
doaj   +3 more sources

Biosynthesis of lactacystin as a proteasome inhibitor [PDF]

open access: yesCommunications Chemistry
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
doaj   +2 more sources

Downregulation of 26S proteasome catalytic activity promotes epithelial-mesenchymal transition. [PDF]

open access: yes, 2016
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

open access: yesBiomolecules, 2022
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
doaj   +1 more source

Proteasome inhibition-enhanced fracture repair is associated with increased mesenchymal progenitor cells in mice.

open access: yesPLoS ONE, 2022
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
doaj   +2 more sources

Synergistic apoptosis induction in leukemic cells by the phosphatase inhibitor salubrinal and proteasome inhibitors. [PDF]

open access: yesPLoS ONE, 2009
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
doaj   +1 more source

Resensitising proteasome inhibitor-resistant myeloma with sphingosine kinase 2 inhibition

open access: yesNeoplasia: An International Journal for Oncology Research, 2022
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
doaj   +1 more source

Microbial proteasomes as drug targets.

open access: yesPLoS Pathogens, 2021
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
doaj   +3 more sources

Proteasome inhibitors

open access: yesBiochemical 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
openaire   +4 more sources

Blocking autophagy overcomes resistance to dual histone deacetylase and proteasome inhibition in gynecologic cancer

open access: yesCell Death and Disease, 2022
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
doaj   +1 more source

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