Global ETD Search
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Showing 1 to 20 of 29 for “"PROTEASOME INHIBITORS"”.
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Synthesis of proteasome inhibitors: analogues of nelfinavir
… effect on chymotrypsin-like activity of 20S proteasome. Previous studies also show the promotion of acceleration of the apoptosis process within cancer cells by inhibition of proteasome activity. Separate experiments proved nelfinavir 1 to be involved in the inhibition of Akt pathway – an …
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Mechanisms Underlying The Heterogeneous Sensitivities of Cancer Cells to Proteasome Inhibitors
<p>The mechanisms underlying cellular response to proteasome inhibitors have not been clearly elucidated in solid tumor models. Evidence suggests that the ability of a cell to manage the amount of proteotoxic stress following proteasome inhibition dictates survival. In this study using the …
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Proteasome Inhibition As A Potential Anti-Breast Cancer Therapy: Mechanisms Of Action And Resistance-Reversing Strategies
<p>AMPK activation and Ubiquitin Proteasome System (UPS) inhibition have gained great attention as therapeutic strategies for the treatment of certain types of cancers. While AMPK serves as a master regulator of cellular metabolism, UPS regulates protein homeostasis. Although the crosstalk between …
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Induction of Caspase-Dependent Death By Proteasome Targeted Therapy In Glioblastoma
… of only 14 months with current treatment. The proteasome inhibitor bortezomib (BTZ) shows efficacy in cancers like myeloma, but its clinical utility in other cancer types has been more limited. Newer proteasome inhibitors such as marizomib (MRZ) have unique inhibitory and death inducing …
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The Major Histocompatibility Complex (MHC) and the proteasome-ubiquitin pathway in T cell development
… molecules in T cell development as well as the proteasome role in antigen processing for MHC-mediated antigen presentation to T cells is well established. However, the contribution of nonclassical MHC molecules, the signals evoked by the MHC-TCR interactions, the signaling role of the …
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Studies on the Cytoplasmic Inclusions Detected in Parkinson's disease
… these aggregates. The presence of ubiquitin and proteasome subunits in these inclusions supports a role for this protein degradation pathway in the processing of proteins involved in this disease. Treatment with proteasome inhibitors resulted in attenuation of degradation and the accumulation of …
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Loperamide enhances bortezomib-mediated cell death in colon cancer cells
… 50 7. Combined treatment with loperamide and proteasome inhibitors does not induce cell death in normal colon cells 56 IV. DISCUSSION 60 V. REFERENCES 64 - 국문요약 - 77
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Integrated cellular, proteomic and metabolite analysis of argyrin B with rational design approaches for immunoproteasome-selective inhibitors
The ubiquitin-proteasome system plays a critical role in cellular protein degradation and homeostasis. Current proteasome inhibitors (PI) present great efficacy against haematologic cancers due to the high secretory load creating an increased dependency on proteostasis, yet resistance and adverse …
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Jab1 Negatively Regulates Pten and Promotes Resistance to Trastuzumab In Her2-Positive Breast Cancer
… degradation of PTEN. Furthermore, I showed that proteasome inhibitors failed to prevent PTEN degradation induced by Jab1 over-expression in breast cancer cells. Instead, the combination of lysosomal protease inhibitors - E64D and pepstatin A - significantly impaired the ability of Jab1 to degrade …
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Biochemical and computational studies towards selective inhibition of the immunoproteasome
The proteasome pathway degrades >90% of cytosolic proteins deemed redundant, misfolded or toxic, thereby influencing key regulatory pathways including: cell cycle control, DNA repair and apoptosis. As such, proteasome inhibitors (PI) have exhibited broad therapeutic applications, particularly for …
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The Role of Linker 2 (L2) Region in RhTRIM5α Assembly and HIV-1 Restriction
… poorly understood mechanism that is sensitive to proteasome inhibitors and/or activation of innate immune signaling pathways. This study focuses on the initial step in restriction that is assembly of TRIM5alpha around the HIV-1 capsid. TRIM5alpha is known to form assemblies in the cytoplasm of the …
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Mechanism of Human Papillomavirus E6-Mediated Repression of P53-Target Gene *Transcription
… human fibrosarcoma HT1080 cells treated with proteasome inhibitors (MG132) and in vitro-assembled chromatin templates reconstituted with purified chromatin assembly factors (Acf1 and ISWI), core histones (H2A, H2B, H3, and H4), and a histone chaperone (NAP-1) in order to define the mechanism …
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Molecular Studies On The Anti-Tumor Effects Of Metal-Based Complexes: Involvement Of The Ubiquitin-Proteasome And Apoptotic Pathways
<p>The ubiquitin-proteasome pathway is crucial to normal cellular function, and as such, has been extensively investigated as a potential target for cancer therapeutics. Many compounds have been tested for their proteasome inhibitory ability, including various small peptide aldehydes, and, …
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PROTEASOME-DEPENDENT ENTRY OF HERPES SIMPLEX VIRUS
… that engages the host cell machinery. The proteasome is a large, ATP-dependent, multisubunit protease that plays a critical role in the maintenance of cell homeostasis. A battery of assays were used to demonstrate that proteasome inhibitors blocked an early step in herpes simplex virus …
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Biochemical Pathways in Apoptosis
… block or delay of Mcl-1 disappearance by either proteasome inhibitors or Mcl-1 over-expression prevents subsequent steps of this apoptotic pathway including the translocation of Bax and Bcl-xL from cytosol to mitochondria and dephosphorylation of BimEL on mitochondria. These sequential events …
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From detection of proteasomal degradation to targeted control of protein depletion
The ubiquitin proteasome system (UPS) regulates protein turnover and catalyzes degradation of misfolded or damaged proteins, thus playing an important role in maintaining protein homoeostasis in eukaryotic cells. The UPS has emerged as a drug target for diverse diseases characterized by altered …
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Rapid turnover of McL-1 couples translation to cell survival and apoptosis
… various cell types. Pre-treatment with several proteasome inhibitors blocked cell death, indicating that the loss of short-lived protein(s) via proteasome-mediated degradation was responsible for cell death. Multiple observations demonstrated that cycloheximide induces cell death by activation …
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Antitumor activity of antimalarials in human breast cancer cells
… addition of quinidine to the growth medium. The proteasome inhibitors, MG-132 and lactacystin completely protected HDAC-1 from the action of quinidine. These data demonstrate that quinidine is a breast tumor cell differentiating agent that causes the loss of HDAC-1 via a proteasomal sensitive …
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PORPHYRIN DERIVATIVES AS VERSATILE PROTEASOME MODULATORS
The ubiquitin proteasome system (UPS) is the primary degradation system in eukaryotic cells, with high selectivity for a myriad of soluble proteins, and perturbations in the UPS are associated with numerous human disorders. For this reason the proteasome has become a pharmacological target for …
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The Role of the Ubiquitin-Proteasome Pathway During Xylem Differentiation in <I>Zinnia elegans</I> Mesophyll Cells and <I>Arabidopsis thaliana</I>
A biochemical characterization of ubiquitin (Ub)-proteasome pathway activity was conducted in <I>Zinnia</I> mesophyll cell cultures to examine potential differences between differentiating cells of tracheary element (TE) cultures and non-differentiating cells of control cultures. The pathway is …
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