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Proteasome Inhibition in Multiple Myeloma: Head-to-Head Comparison of Currently Available Proteasome Inhibitors [PDF]
Cell Chemical Biology, 2019 Proteasome inhibitors (PIs) are a backbone of multiple myeloma (MM) therapy. The proteasome harbors six proteolytically active subunits (β1, β2, β5), while β5 was identified as rate-limiting and is a primary target of clinically available PIs.
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Proteasomes and proteasome inhibition in the central nervous system
Free Radical Biology and Medicine, 2001Although the proteasome is responsible for the majority of intracellular protein degradation, and has been demonstrated to play a pivotal role in a diverse array of cellular activities, the role of the proteasome in the central nervous system is only beginning to be elucidated.
Q, Ding, J N, Keller
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An Historic Perspective of Proteasome Inhibition
Seminars in Hematology, 2012The ubiquitin-proteasome system (UPS) and associated signaling pathways are regarded today as an exciting area of development for novel therapeutics. However, two decades ago, following the discovery and elucidation of ubiquitin and the 26S proteasome as key mediators of protein turnover, the concept of inhibiting the UPS was not even considered a ...
Dixie-Lee, Esseltine, George, Mulligan
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Proteasome inhibition in multiple myeloma
European Journal of Cancer, 2006The ubiquitin-proteasome pathway is the major cellular degradative system for various proteins critical for proliferation, survival and homing of myeloma cells. Bortezomib is the first specific and reversible proteasome inhibitor for clinical application in humans.
Martin, Kropff +4 more
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Rapamycin Allosterically Inhibits the Proteasome
Molecular Pharmacology, 2013Rapamycin is a canonical allosteric inhibitor of the mammalian tarpet of rapamycin (mTOR) kinase with immunosuppressive and proapoptotic activities. We found that in vitro rapamycin also regulates the proteasome, which is an essential intracellular protease of the ubiquitin-proteasome pathway.
Pawel A, Osmulski, Maria, Gaczynska
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Proteasome inhibition by peptide-semicarbazones
Bioorganic & Medicinal Chemistry, 2008Peptide-semicarbazones derived from Z-Trp-Trp-Phe-aldehyde inhibit the chymotryptic activity of the human proteasome at nanomolar concentrations, but are less active in a NFkappaB reporter gene assay. Cyclic semicarbazones, in contrast, combine a strong inhibitory effect on the enzyme with an inhibition of NFkappaB signaling in the nanomolar range.
Johann, Leban +5 more
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Structural Investigation of Proteasome Inhibition
Biological Chemistry, 1997The novel proteolytic mechanism of the 20S proteasome from T. acidophilum has been investigated by X-ray crystallography using small-molecule inhibitors and substrate analogues. The 20S proteasome degrades unfolded substrates into small peptides of a defined length. Calpain inhibitor II, chymostatin and lactacystin all bind in the previously identified
L, Ditzel, D, Stock, J, Löwe
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Rapamycin inhibits proteasome activator expression and proteasome activity
European Journal of Immunology, 1997AbstractRapamycin (RAPA) is a potent immunosuppressive drug, and certain of its direct or indirect targets might be of vital importance to the regulation of an immune response. In this study, we used differential hybridization to search for human genes whose expression was sensitive to RAPA. Seven RAPA‐sensitive genes were found and one of them encoded
X, Wang +6 more
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Targeting the Ubiquitin Proteasome System: Beyond Proteasome Inhibition
Current Pharmaceutical Design, 2013The Ubiquitin-Proteasome System (UPS) has been considered as privileged pharmacological target for drug development due to the tremendous potential for intervention on multiple pathologies including cancer, neurodegenerative diseases, immune diseases and multiple infections.
Wendy, Xolalpa +3 more
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