proteasome inhibitors
Increased resistance to proteasome inhibitors in multiple myeloma mediated by cIAP2 - implications for a combinatorial treatment
... XIAP has been described to inhibit caspase-3, -7 and -9 via its BIR2 and BIR3 domain and is therefore considered mediating the anti-apoptotic effect via this mechanism [16]. The results from the PLA studies suggest that ...
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The use of proteasome inhibitors in anti-cancer therapy
... 26S proteasome, thanks to its prior labeling with a poly-ubiquitin ...ubiquitin- proteasome complex is involved in the control of many important cellular ...Specific proteasome inhibitors are ...
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Therapeutic targeting of cancer cell cycle using proteasome inhibitors
... with proteasome inhibition activity has been tested and recognized as potential anti- cancer drugs against hematological malignancies and some solid cancers ...having proteasome inhibitory activity have ...
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Synthetic Analogs of Green Tea Polyphenols as Proteasome Inhibitors
... cal proteasome inhibitors and the cancer-preventive effects of green tea ...as proteasome inhibitors and potential cancer-preventive agents prompted our current ...the proteasome or ...
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Proteasome inhibitors modulate anticancer and anti-proliferative properties via NF-kB signaling, and ubiquitin-proteasome pathways in cancer cell lines of different organs
... that proteasome inhibitors and small interfering RNA-mediated knockdown of the proteasome’s enzymatic subunits promoted auto phagosome formation as also ob- served in present ...displaying proteasome ...
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Suppression of nitric oxide induction and pro-inflammatory cytokines by novel proteasome inhibitors in various experimental models
... the proteasome is a pivotal regulator of inflammation, which modulates the induction of inflammatory mediators such as TNF-a IL-1, IL-6, and nitric oxide (NO) in response to a variety of ...non-toxic ...
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Budding of Equine Infectious Anemia Virus Is Insensitive to Proteasome Inhibitors
... To further explore the requirements of Ub in retrovirus budding, we decided to test the sensitivity of equine infectious anemia virus (EIAV) to proteasome inhibitors. This study was of interest because EIAV ...
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Synergistic effects of combining proteasome inhibitors with chemotherapeutic drugs in lung cancer cells
... the proteasome complex and degradation of the proteins into small ...and proteasome inhibitors (PIs) have significant preclinical and clinical activity in several cancers, especially in combination ...
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Mechanism of pharmacophore biosynthesis for epoxyketone proteasome inhibitors
... α,β-epoxyketone proteasome inhibitor TMC-86A from Streptomyces ...epoxyketone proteasome inhibitors with stereochemistry where known, arranged chronologically, with predicted or confirmed ...26S ...
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Mechanistic Insights into the Enhancement of Adeno-Associated Virus Transduction by Proteasome Inhibitors
... whether proteasome inhibition is sufficient for en- hancement of rAAV transduction in ...the proteasome inhibitors at this dose ...that proteasome inhibition is sufficient for the enhancement ...
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Towards subunit specific proteasome inhibitors
... selective proteasome inhibitors, their vinyl sulfone counterparts and their biological analysis by the competition assay in HEK293T and EL4 lysates as well as fluorogenic peptide hydroly- sis assay with ...
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Comprehensive study of proteasome inhibitors against Plasmodium falciparum laboratory strains and field isolates from Gabon
... strategies. Proteasome inhibi- tors are in the focus of drug development for various dis- eases and candidates have already entered clinical trials ...single proteasome inhibitor as a drug development ...
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Radiosensitization of noradrenaline transporter-expressing tumour cells by proteasome inhibitors and the role of reactive oxygen species
... of proteasome inhibition as a means of enhancing radiation-induced cancer cell kill, especially when given in combination with the radiophar- maceutical 131 I-MIBG for the targeted radiotherapy of ...alternative ...
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Selective growth inhibition of human malignant melanoma cells by syringic acid-derived proteasome inhibitors
... Syringic acid derivatives 2, 5 and 6 were shown to inhibit human malignant cell growth, and proteasome activity, and apoptosis inducers. Proteasome inhibitors are considered promising anticancer ...
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Suberoyl bis-hydroxamic acid enhances cytotoxicity induced by proteasome inhibitors in breast cancer cells
... Methods: MCF-7 and MDA-MB-231 breast cancer cells were treated with SBHA, Bortezomib, and MG-132 alone or in combination for 72 h. Cell proliferation, colony formation, apoptosis and gene expression changes were ...
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PROTEASOME INHIBITORS FOR USE IN MULTIPLE MYELOMA
... first-in-class proteasome inhibitor bortezomib in 2003, made possible the therapeutic validation of proteasome as a target for use in discovery and development of new treatment options in cancer, ...
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CCR10/CCL27 crosstalk contributes to failure of proteasome- inhibitors in multiple myeloma
... Primary stroma cells isolated from three myeloma patients also rescued myeloma cell lines Figure 2B, and survival of CD138-sorted primary myeloma cells from four patients seeded on HS-5 [r] ...
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Proteasome inhibitors act as bifunctional antagonists of human immunodeficiency virus type 1 latency and replication
... combinatorial chemistry between different HIV-1 latency activators and replication inhibitors to create novel clas- ses of bifunctional HIV-1 antagonists. However, a PI may very well be a viable option for ...
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Trypanosoma brucei: β2-selective proteasome inhibitors do not block the proteasomal trypsin-like activity but are trypanocidal
... LU inhibitors was performed with extracts from bloodstream forms of ...the proteasome (Fig. 1B-E). At 10 µM, none of the inhibitors affected the activity of the trypsin-like activity of the ...
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Proteasome inhibitors as experimental therapeutics of autoimmune diseases
... increased proteasome activity and that this feature would render them particularly sus- ceptible to proteasome inhibition and accumulation of polyubiquitinated proteins, eliciting an apoptotic ...to ...
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