Results 11 to 20 of about 107,234 (254)
Proteasome Inhibitors: Harnessing Proteostasis to Combat Disease
Molecules, 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
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Biochemical Pharmacology, 2015 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
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Biomolecules, 2020 Currently, proteasome inhibitors bortezomib, carfilzomib, and ixazomib are successfully used in clinics to treat multiple myeloma. However, these agents show limited efficacy against solid tumors. Identification of drugs that can potentiate the action of
Janakiram R. Vangala +2 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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Microbial proteasomes as drug targets.
PLoS Pathogens, 2021 Proteasomes are compartmentalized, ATP-dependent, N-terminal nucleophile hydrolases that play essentials roles in intracellular protein turnover. They are present in all 3 kingdoms.
Hao Zhang, Gang Lin
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Postnatal proteasome inhibition induces neurodegeneration and cognitive deficiencies in adult mice: a new model of neurodevelopment syndrome. [PDF]
PLoS ONE, 2011 Defects in the ubiquitin-proteasome system have been related to aging and the development of neurodegenerative disease, although the effects of deficient proteasome activity during early postnatal development are poorly understood.
Rocío Romero-Granados +3 more
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Molecules, 2022 Proteasome inhibitors have shown relevant clinical activity in several hematological malignancies, namely in multiple myeloma and mantle cell lymphoma, improving patient outcomes such as survival and quality of life, when compared with other therapies ...
Carlota Leonardo-Sousa +7 more
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Proteasome inhibitors alter levels of intracellular peptides in HEK293T and SH-SY5Y cells. [PDF]
PLoS ONE, 2014 The proteasome cleaves intracellular proteins into peptides. Earlier studies found that treatment of human embryonic kidney 293T (HEK293T) cells with epoxomicin (an irreversible proteasome inhibitor) generally caused a decrease in levels of intracellular
Sayani Dasgupta +6 more
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Blood Cancer Journal, 2020 Protein homeostasis is critical for maintaining eukaryotic cell function as well as responses to intrinsic and extrinsic stress. The proteasome is a major portion of the proteolytic machinery in mammalian cells and plays an important role in protein ...
Yanyan Gu +9 more
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Paradoxical inhibition of cellular protein expression by proteasome inhibitors
Biomolecular Concepts, 2012 Proteasome inhibitors are used as anticancer drugs, however, the precise mechanisms of their selective activity against cancer cells are not understood well.
Gartel Andrei L.
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