Haematologica, 2013 The ex vivo sensitivity of pediatric leukemia cells to the proteasome inhibitor bortezomib was compared to 3 next generation proteasome inhibitors: the epoxyketone-based irreversible proteasome inhibitors carfilzomib, its orally bio-available analog ONX ...
Denise Niewerth +13 more
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The capture proteasome assay (CAPA) to evaluate subtype-specific proteasome inhibitors
Data in Brief, 2015 We recently developed a new assay to measure proteasome activity in vitro (CAPA for capture proteasome assay) [1], based on proteasome capture on an antibody-coated plate.
Nathalie Vigneron +2 more
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Homopiperazine derivatives as a novel class of proteasome inhibitors with a unique mode of proteasome binding. [PDF]
PLoS ONE, 2013 The proteasome is a proteolytic machinery that executes the degradation of polyubiquitinated proteins to maintain cellular homeostasis. Proteasome inhibition is a unique and effective way to kill cancer cells because they are sensitive to proteotoxic ...
Jiro Kikuchi +11 more
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Rational design of novel phenol ether derivatives as non-covalent proteasome inhibitors through 3D-QSAR, molecular docking and ADMET prediction [PDF]
Exploration 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
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Computational Approaches for the Discovery of Human Proteasome Inhibitors: An Overview
Molecules, 2016 Proteasome emerged as an important target in recent pharmacological research due to its pivotal role in degrading proteins in the cytoplasm and nucleus of eukaryotic cells, regulating a wide variety of cellular pathways, including cell growth and ...
Romina A. Guedes +3 more
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Mutant p53–Nrf2 axis regulates the proteasome machinery in cancer
Molecular & Cellular Oncology, 2017 The proteasome machinery is a common target of gain-of-function p53 missense mutants. Upregulation of the proteasome fosters chemoresistance to proteasome inhibitors.
Kamil Lisek +2 more
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Different degree in proteasome malfunction has various effects on root growth possibly through preventing cell division and promoting autophagic vacuolization. [PDF]
PLoS ONE, 2012 The ubiquitin/proteasome pathway plays a vital role in plant development. But the effects of proteasome malfunction on root growth, and the mechanism underlying this involvement remains unclear.
Xianyong Sheng +5 more
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The ubiquitin‐proteasome pathway and proteasome inhibitors [PDF]
Medicinal Research Reviews, 2001 AbstractThe ubiquitin‐proteasome pathway has emerged as a central player in the regulation of several diverse cellular processes. Here, we describe the important components of this complex biochemical machinery as well as several important cellular substrates targeted by this pathway and examples of human diseases resulting from defects in various ...
J, Myung, K B, Kim, C M, Crews
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Chemical proteasome inhibition as a novel animal model of inner retinal degeneration in rats.
PLoS 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
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Marine 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
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