Results 11 to 20 of about 949,070 (290)
AbstractProteasome inhibitors are indispensable research tools in immunology and cell biology. With numerous proteasome inhibitors available commercially, choosing the appropriate compound for a biological experiment may be challenging, especially for a novice. This unit provides an overview of the proteasome inhibitors commonly used in research.
Downey, S.L. +3 more
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The capture proteasome assay (CAPA) to evaluate subtype-specific proteasome inhibitors [PDF]
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
doaj +2 more sources
Hydroxyureas as Noncovalent Proteasome Inhibitors
Inhibitors with a new mechanism of action are needed for 20S proteasome (CP) inhibition owing to the ineffectiveness of current market drugs against some types of solid tumors. A novel class of nonpeptidic CP inhibitors has been developed, which display reversible and noncovalent binding.
Gallastegui, Nerea +5 more
openaire +6 more sources
Homopiperazine derivatives as a novel class of proteasome inhibitors with a unique mode of proteasome binding. [PDF]
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
doaj +2 more sources
Computational Approaches for the Discovery of Human Proteasome Inhibitors: An Overview
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
doaj +2 more sources
Joining the Army of Proteasome Inhibitors
An article in this issue of Chemistry & Biology (Hines et al., 2008) and a recent study in Nature (Groll et al., 2008) establish three natural products as novel proteasome inhibitors. These inhibitors, discovered in an unusual way, reveal a different mechanism of proteasome inhibition and suggest new therapeutic application of its inhibitors.
Kisselev, Alexei F.
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Proteasome Inhibitors in Waldenström Macroglobulinemia
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
core +7 more sources
New proteasome inhibitors in the treatment of multiple myeloma
The treatment of patients with relapsed and/or refractory multiple myeloma has improved considerably in the last 15 years, after the introduction of proteasome inhibitors and immunomodulatory drugs.
Vania Tietsche de Moraes Hungria +9 more
doaj +2 more sources
Cardiovascular toxicity of proteasome inhibitors in multiple myeloma therapy
The treatment for multiple myeloma has advanced significantly over the past few decades. Proteasome inhibitors have become the cornerstone of the treatment of multiple myeloma.
Huang, Shan +6 more
core +2 more sources
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

