The novel 2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells
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چکیده
منابع مشابه
Bortezomib / proteasome inhibitor PS - 341 resistance in multiple myeloma
198 words; Text4628 words Blood First Edition Paper, prepublished online June 24, 2004; DOI 10.1182/blood-2004-02-0547 Copyright (c) 2004 American Society of Hematology only. For personal use at PENN STATE UNIVERSITY on February 23, 2013. bloodjournal.hematologylibrary.org From
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HIV protease inhibitors (HIV-PI) are oral drugs for HIV treatment. HIV-PI have antitumor activity via induction of ER-stress, inhibition of phospho-AKT (p-AKT) and the proteasome, suggesting antimyeloma activity. We characterize the effects of all approved HIV-PI on myeloma cells. HIV-PI were compared regarding cytotoxicity, proteasome activity, ER-stress induction and AKT phosphorylation using...
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Bortezomib (PS-341), a selective inhibitor of proteasomes, induces apoptosis in multiple myeloma (MM) cells; however, prolonged drug exposure may result in cumulative toxicity and the development of chemoresistance. Here we show that combining PK-11195 (PK), an antagonist to mitochondrial peripheral benzodiazepine receptors (PBRs), with bortezomib triggers synergistic anti-MM activity even in d...
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Although the incidence of multiple myeloma (MM) is increasing, the median overall survival and the number of agents in the pipeline for treating MM also are increasing. Response rates higher than 80% are not uncommon in the frontline setting when the novel agents thalidomide, lenalidomide, and bortezomib are used in combination. Response rates and survival also have improved in disease that has...
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The proteasome plays a vital role in the degradation of proteins involved in several pathways including the cell cycle, cellular proliferation and apoptosis and is a validated target in cancer treatment. Bortezomib (Velcade®, PS-341) is the first US FDA approved proteasome inhibitor anticancer drug used in the treatment of refractory multiple myeloma. In spite of its improved efficacy compared ...
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ژورنال
عنوان ژورنال: Haematologica
سال: 2015
ISSN: 0390-6078,1592-8721
DOI: 10.3324/haematol.2014.109421