Results 11 to 20 of about 1,442,074 (300)
Structural Characterization of Proteasome Inhibition [PDF]
, 2022 The proteasome plays a major role in non-lysosomal protein degradation pathways and inhibition of proteasomes became a valid therapeutic strategy for anti-cancer therapy in the recent years. Current efforts focus on the identification and development of second generation inhibitors with enhanced pharmacological properties. For this, improved structural
Schrader, Jil +4 more
openaire +5 more sources
Inhibition of Proteasome Activity Induces Formation of Alternative Proteasome Complexes [PDF]
Journal of Biological Chemistry, 2016 The proteasome is an intracellular protease complex consisting of the 20S catalytic core and its associated regulators, including the 19S complex, PA28αβ, PA28γ, PA200, and PI31. Inhibition of the proteasome induces autoregulatory de novo formation of 20S and 26S proteasome complexes. Formation of alternative proteasome complexes, however, has not been
Welk, Vanessa +6 more
core +6 more sources
Exploring the proteasome system: A novel concept of proteasome inhibition and regulation
Pharmacology & Therapeutics, 2020 The proteasome is a well-identified therapeutic target for cancer treatment. It acts as the main protein degradation system in the cell and degrades key mediators of cell growth, survival and function. The term "proteasome" embraces a whole family of distinct complexes, which share a common proteolytic core, the 20S proteasome, but differ by their ...
Wang, X., Meul, T., Meiners, S.
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Proteasome inhibition for the treatment of glioblastoma [PDF]
Expert Opinion on Investigational Drugs, 2020 INTRODUCTION Glioblastoma is a primary brain tumor with a poor prognosis despite multimodal therapy including surgery, radiotherapy and alkylating chemotherapy. Novel therapeutic options are therefore urgently needed; however, there have been various drug failures in late-stage clinical development.
Roth, Patrick +3 more
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Proteasome Inhibition in the Treatment of Cancer [PDF]
Cell Cycle, 2004 The proteasome is the main extralysosomal system involved in intracellular proteolysis. A number of proteasome substrates, including cyclins, IkappaB, and p53, are critical to cell cycle progression and apoptosis. Interruption of the degradation of these substrates through proteasome inhibition is a novel and unique approach to the treatment of ...
Paul G, Richardson +3 more
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Bivalency as a principle for proteasome inhibition [PDF]
Proceedings of the National Academy of Sciences, 1999 The proteasome, a multicatalytic protease, is known to degrade unfolded polypeptides with low specificity in substrate selection and cleavage pattern. This lack of well-defined substrate specificities makes the design of peptide-based highly selective inhibitors extremely difficult.
G, Loidl +4 more
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Exploring the role and clinical implications of proteasome inhibition in medulloblastoma [PDF]
, 2021 Ubiquitin proteasome-mediated protein degradation has been implicated in posttranslational oncogenesis in medulloblastoma. Current research is evaluating the clinical implications of proteasome inhibition as a therapeutic target.
Pulley, Michelle D +9 more
core +1 more source
iScience, 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
Fluorescence-based proteasome activity profiling [PDF]
, 2011 With the proteasome emerging as a therapeutic target for cancer treatment, accurate tools for monitoring proteasome (inhibitor) activity are in demand.
Jong, A. +9 more
core +1 more source
Haematologica, 2015 Proteasome inhibitor resistance is a challenge for myeloma therapy. Bortezomib targets the β5 and β1 activity, but not the β2 activity of the proteasome.
Marianne Kraus +15 more
doaj +1 more source