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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

The proteasome: A key modulator of nervous system function, brain aging, and neurodegenerative disease

open access: yesFrontiers in Cell and Developmental Biology, 2023
The proteasome is a large multi-subunit protease responsible for the degradation and removal of oxidized, misfolded, and polyubiquitinated proteins. The proteasome plays critical roles in nervous system processes.
Kanisa Davidson, Andrew M. Pickering
doaj   +1 more source

Oleuropein Activates Neonatal Neocortical Proteasomes, but Proteasome Gene Targeting by AAV9 Is Variable in a Clinically Relevant Piglet Model of Brain Hypoxia-Ischemia and Hypothermia

open access: yesCells, 2021
Cerebral hypoxia-ischemia (HI) compromises the proteasome in a clinically relevant neonatal piglet model. Protecting and activating proteasomes could be an adjunct therapy to hypothermia.
Nagat El Demerdash   +6 more
doaj   +1 more source

The 20S as a stand-alone proteasome in cells can degrade the ubiquitin tag

open access: yesNature Communications, 2021
The proteasome, the primary protease for ubiquitin-dependent proteolysis in eukaryotes, is usually found as a mixture of 30S, 26S, and 20S complexes. These complexes have common catalytic sites, which makes it challenging to determine their distinctive ...
Indrajit Sahu   +14 more
semanticscholar   +1 more source

Enhanced O-GlcNAcylation Mediates Cytoprotection under Proteasome Impairment by Promoting Proteasome Turnover in Cancer Cells

open access: yesiScience, 2020
Summary: The proteasome is a therapeutic target in cancer, but resistance to proteasome inhibitors often develops owing to the induction of compensatory pathways.
Eiichi Hashimoto   +7 more
doaj   +1 more source

Ubiquitin–proteasome system (UPS) as a target for anticancer treatment

open access: yesArchives of pharmacal research, 2020
The ubiquitin–proteasome system (UPS) plays an important role in the cellular processes for protein quality control and homeostasis. Dysregulation of the UPS has been implicated in numerous diseases, including cancer.
Jinyoung Park, Jinhong Cho, E. J. Song
semanticscholar   +1 more source

Targeted Protein Degradation: Principles and Applications of the Proteasome

open access: yesCells, 2023
The proteasome is a multi-catalytic protease complex that is involved in protein quality control via three proteolytic activities (i.e., caspase-, trypsin-, and chymotrypsin-like activities).
Yosup Kim   +4 more
doaj   +1 more source

Proteasome Inhibitors for the Treatment of Multiple Myeloma

open access: yesCancers, 2020
Use of proteasome inhibitors (PIs) has been the therapeutic backbone of myeloma treatment over the past decade. Many PIs are being developed and evaluated in the preclinical and clinical setting.
S. Ito
semanticscholar   +1 more source

Proteasome Inhibitor Drugs.

open access: yesAnnual Review of Pharmacology and Toxicology, 2020
Proteasomes are large, multicatalytic protein complexes that cleave cellular proteins into peptides. There are many distinct forms of proteasomes that differ in catalytically active subunits, regulatory subunits, and associated proteins.
L. Fricker
semanticscholar   +1 more source

Wiggle and Shake: Managing and Exploiting Conformational Dynamics during Proteasome Biogenesis

open access: yesBiomolecules, 2023
The 26S proteasome is the largest and most complicated protease known, and changes to proteasome assembly or function contribute to numerous human diseases.
Daniel Betancourt   +2 more
doaj   +1 more source

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