Results 31 to 40 of about 107,234 (254)

Rational design of novel phenol ether derivatives as non-covalent proteasome inhibitors through 3D-QSAR, molecular docking and ADMET prediction [PDF]

open access: yesExploration of Drug Science, 2023
Aim: The purpose of this paper is to use different structures and ligand-based drug design methods properly to provide theoretical guidance for the design of novel non-covalent proteasome inhibitors, and conduct theoretical analysis of the binding ...
Miao Yuan   +4 more
doaj   +1 more source

Chemical proteasome inhibition as a novel animal model of inner retinal degeneration in rats.

open access: yesPLoS ONE, 2019
Chemical proteasome inhibition has been a valuable animal model of neurodegeneration to uncover roles for the ubiquitin-proteasome system in the central nervous system.
Masaaki Kageyama   +4 more
doaj   +1 more source

A High-Content Screening Assay for the Discovery of Novel Proteasome Inhibitors from Formosan Soft Corals

open access: yesMarine Drugs, 2018
The ubiquitin-proteasome system (UPS) is a major proteolytic pathway that safeguards protein homeostasis. The main 26S proteasome consists of a 20S catalytic core proteasome and a 19S substrate recognition proteasome.
Xue-Hua Ling   +4 more
doaj   +1 more source

The Proteasome Activator PA200/PSME4: An Emerging New Player in Health and Disease

open access: yesBiomolecules, 2022
Proteasomes comprise a family of proteasomal complexes essential for maintaining protein homeostasis. Accordingly, proteasomes represent promising therapeutic targets in multiple human diseases.
Ayse Seda Yazgili   +2 more
doaj   +1 more source

Proteasome Inhibitors in Waldenström Macroglobulinemia

open access: yesHematology/Oncology Clinics of North America, 2018
Waldenström macroglobulinemia (WM) remains an incurable B-cell lymphoproliferative disorder, yet therapy is only considered for patients with symptomatic disease. Primary therapy options for WM include combinations based on anti-CD20 monoclonal antibodies, mainly rituximab. However, proteasome inhibitors have become an important part of WM therapy both
Kastritis, Efstathios   +1 more
openaire   +5 more sources

Clinical Use of Proteasome Inhibitors in the Treatment of Multiple Myeloma

open access: yesPharmaceuticals, 2014
Multiple myeloma (MM) is an incurable hematological malignancy characterized by the clonal proliferation of neoplastic plasma cells. The use of proteasome inhibitors in the treatment of MM has led to significant improvements in outcomes.
Noah M. Merin, Kevin R. Kelly
doaj   +1 more source

Proteasome inhibitors for multiple myeloma [PDF]

open access: yesJapanese Journal of Clinical Oncology, 2018
Therapeutic strategies for multiple myeloma have dramatically changed in the last two decades, especially after the introduction of proteasome inhibitors. The first-in-class proteasome inhibitor, bortezomib, was approved by the US Food and Drug Administration in 2003.
Kiyoshi, Okazuka, Tadao, Ishida
openaire   +2 more sources

The ubiquitin‐proteasome system and autophagy as guardians of the cellular proteome

open access: yesFEBS Letters, EarlyView.
This Perspective covers the three principles governing the crosstalk between the ubiquitin‐proteasome system and autophagy in cellular proteostasis: (1) a shared ubiquitin code routing substrates via shuttle factors or autophagy receptors; (2) spatial compartmentalization into phase‐separated degradation hubs and organelle‐specific modules (exemplified
Ivan Dikic
wiley   +1 more source

Microbiome−host proteostasis crosstalk—An emerging perspective on mechanisms and interventions toward healthy longevity

open access: yesFEBS Letters, EarlyView.
Proteostasis and the gut microbiota play a key role in shaping host physiology. Microbiota‐derived metabolites, vitamins, and RNA modulate host proteostasis. Findings from model systems, including C. elegans, indicate microbes can either stabilize or disrupt host proteostasis.
Abhishek Anil Dubey, Maria Ermolaeva
wiley   +1 more source

Small interfering RNA targeting mcl-1 enhances proteasome inhibitor-induced apoptosis in various solid malignant tumors

open access: yesBMC Cancer, 2011
Background Targeting the ubiquitin-proteasome pathway is a promising approach for anticancer strategies. Recently, we found Bik accumulation in cancer cell lines after they were treated with bortezomib.
Zhou Wei   +6 more
doaj   +1 more source

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