Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 32 for “"Procaspase"”.
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The discovery and characterization of anticancer procaspase activating compounds
… inactive or aberrantly expressed. Paradoxically, procaspases are generally upregulated and rarely mutated in cancers. Therefore, a small molecule that directly activates executioner procaspase-3/-7 to caspase-3/-7 to induce apoptosis in cancer cells could circumvent the defective apoptotic …
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Small molecule activators of procaspase-3 as an anticancer strategy
… levels of key proteins. The apoptotic protein procaspase-3 has been shown to be upregulated in a variety of cancer cell types and plays a pivotal role in the execution of apoptosis. As such, the reactivation of the apoptotic cascade through small molecule activators of procaspase-3 is an …
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Investigating procaspase-3 as a potential therapeutic target in canine osteosarcoma
… investigates the use of PAC-1, a newly developed procaspase-3 activating compound, in the treatment of canine osteosarcoma. Procaspase-3 is expressed in osteosarcoma cells, and furthermore, greater expression is seen in malignant canine osteoblasts than normal osteoblasts. Exposing cells to PAC-1 …
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Procaspase-3 activation as a strategy to overcome resistance to targeted anticancer therapies
… the zymogen of the executioner caspase, procaspase-3, rather than being downregulated in cancer, has been found to be overexpressed in many cancers. In Chapter 1, I will describe the list of cancers that overexpress procaspase-3, before rationalizing this paradoxical observation. Finally, …
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Evaluation of therapy for canine intracranial neoplasia using PAC-1, a novel and potent procaspase-3 activator
… pro-apoptotic small molecule activator of procaspase-3 (PC-3), with orphan drug status for the treatment of human glioblastoma multiforme. PC-3 is frequently overexpressed in malignantly transformed tissues, providing an opportunity to selectively induce apoptosis in cancer cells with …
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The Modulation of Life and Death: Small Molecule Activators and Inhibitors of Necrotic and Apoptotic Pathways
… major projects focus on the direct activation of procaspase-3 and the inhibition of poly(ADP-ribose) glycohydrolase (PARG). Through the development of high-throughput screens, a small molecule activator of procaspase-3 (PAC-1) and an inhibitor of PARG (PIP-1) were identified. PAC-1 was shown to …
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Zelluläre Regulation von Leben und Tod durch Todeseffektordomänen (DED)-enthaltende Proteine: CAP3, c-FLIP R und p22-FLIP
… DED-enthaltenden Proteinen gehören u.a. Procaspase-8 und -10, während die c-FLIPs (engl.: cellular FLICE inhibitory proteins) zu den wichtigsten anti-apoptotischen DED-enthaltenen Proteinen gehören. Das CD95-vermittelte Todessignal wird nach Aktivierung des Rezeptors durch Anlagerung von …
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Characterization of the Anti-Inflammatory Effects of the Molluscum Contagiosum Virus MC160 Protein
… that the second DED of MC160 interacts with procaspase-8 as a means to inhibit NF-kappaB activation, while the C-terminus of MC160 interacts with the chaperone Hsp90. Because both procaspase-8 and Hsp90 associate with the IKK complex, we believe that the MC160 protein binds these proteins as …
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Small Molecule Modulation of Caspase Enzymatic Activity
… in vitro mechanism of a previously identified procaspase-3 activator, PAC-1, was conducted. Through enzymatic assays under various buffer conditions, the in vitro mechanism of PAC-1 activation of procaspase-3 was conclusively found to be through relief of enzyme inhibition by metal ions. Zinc, …
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Development of PAC-1 as a privileged agent for combination chemotherapy
… alterations. Small-molecule activation of procaspase-3 represents a particularly promising opportunity, based upon its determinant role in the execution of apoptosis and its widespread over-expression across many diverse cancer types. PAC-1 is a small-molecule that facilitates procaspase-3 …
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Investigating couplet strategies incorporating 4 pillars of cancer therapy
… tumors in dogs. Chapter III introduces the procaspase-3 activator, PAC-1, which can selectively induce apoptosis in cancerous cells by leveraging the overexpression of procaspase-3. Exploiting procaspase-3 overexpression by cancer cells is thought to explain why PAC-1 can synergize with …
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Pre-clinical evaluation of inhibitors of apoptosis protein (IAP) antagonists in colorectal cancer
… complex consisting of RIPK1, FADD and procaspase-8. Procaspase-8 undergoes homodimerization within this complex and subsequently activates effector caspases-3 and -7 to promote apoptosis. FLIP, a pseudo-caspase, can also bind to FADD and inhibit homodimerization of procaspase-8, …
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Development of a Modular Anti-HIV Transducer Protein
… protein structure capable of activating procaspase 8 and procaspase 9, thus leading to apoptosis. The anti-HIV transducer can be used to treat the cells actively infected with HIV. We have prepared the anti-HIV transducers and demonstrated that they induce apoptosis in the presence of HIV …
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Apoptosis Pathways: Presence and significance in Ejaculated Human Spermatozoa
… <p>In immunoblots, the presence of procaspase-3 was detected in high and low motility fractions from donors and patients. Active caspase-3 was detected in high and low motility fractions from donors and patients. Procaspase-7, but not active, was also detected. Procaspase-9 was …
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Post-translational modifications of c-FLIP: opportunities for therapeutic intervention
… two tandem death effector domains, homologous to procaspase-8. FLIP preferentially binds to FADD via its DEDs, inhibiting the recruitment and processing of procaspase-8 to its active form. Normal cells are resistant to loss of FLIP, but cancer cells are not. Targeting FLIP in cancer is an …
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Influence of Human Papillomavirus 16 E6 on TRAIL-Mediated Apoptosis
… reduction in the protein levels of both FADD and procaspase-8, which results in suppression of the activation of caspases 8, 3 and 2. Interestingly, E6 does not interfere with the mitochondrial apoptotic pathway even though HCT116 cells have been classified as type II cells with regard to TRAIL …
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Investigating Apoptosis Pathway In Chronic Lymphocytic Leukemia: Stromal Influence and Therapeutic Activation
… and directly activate terminal executioner procaspases to induce apoptosis was investigated. Executioner procaspase activities are blocked by zinc and zinc removal releases this inhibition. CLL primary cells express high levels of executioner procaspases-7 and -3 compared to normal …
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Intracellular delivery of rabbit monoclonal antibody
… inside cytoplasm, three RabMAbs against actin, procaspase-3 and NF-κB respectively were studied. Their binding activities after delivery were verified via sandwich-ELISA data. The immunofluorescent staining of the delivered RabMAb against actin showed it specifically bound to the actin filament …
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HMG-CoA Reductase Inhibitors Act Synergistically with UCN-01 Through RAS Inhibition
… 18 hours) resulted in mitochondria dysfunction, procaspase 3 and 9 cleavage, and PAW degradation along with marked cytochrome C release and apoptosis. Although similar molecular mechanisms have not yet been confirmed in other cancers, our hypothesis holds that enhanced apoptotic effects of UCN-01 …
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Estrogen Receptor -Dependent and Estrogen Receptor-Independent Pathways for Tamoxifen and 4-Hydroxytamoxifen-Induced Programmed Cell Death
… apoptosis appears to be at the level of procaspase 9 activation. This study describes a unique ER-dependent, programmed cell death-promoting activity of TAM and OHT that is distinct from their ability to compete with estrogens for binding to the ER.
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