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Showing 1 to 18 of 18 for “"procaspase-3"”.
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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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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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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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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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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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Impact of delta-tocotrienol on human melanoma cell proliferation
… of cyclin-dependent kinase 4. Concomitantly, procaspase-3 cleavage and morphological changes detected by fluorescence microscopy following acridine orange and ethidium bromide dual staining showed d-δ-tocotrienol-induced apoptosis in melanoma cells. Consequent to mevalonate deprivation and the …
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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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Nucleic Acid Scaffold-dependent Proximity-mediated Enzyme Response (NASPER) - A Proof of Concept Study
… hTERT mRNA in HeLa cells. No cleavage of a procaspase-3 construct could be detected in apoptosis assays in Chapter 8, and further work is required to elucidate the cause. Chapter 9 describes further experiments to understand the binding characteristics of designed PUF domains using …
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Improving the process synthesis, potency, and pharmacokinetics of the anticancer compound PAC-1
Embargo set by: Seth Robbins for item 89526 Lift date: 2017-09-29T21:08:35Z Reason: Author requested closed access (OA after 2yrs) in Vireo ETD system
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Molecular Mechanisms Involved In Krabbe's Disease
… modelli cellulari impiegati la proteolisi della procaspase-3, l aumento di espressione di Bad e di p53 e l attenuazione dell attivazione di NF-kB. Gli effetti più severi sono stati registrati nei precursori degli oligodendrociti piuttosto che nei fibroblasti. La presente ricerca ha dimostrato, …
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Formation of caspase activating complexes and activation of caspase-12 during apoptosis in AKR-2B mouse fibroblasts
… Fusionskonstruktes in AKR-2B Zellen wurde die Procaspase-3 im Cytoplasma lokalisiert, während die aktive Caspase-3 vorwiegend in membranumhüllten Vesikeln und zum Teil im Cytoplasma aktiviert wurde. Ebenfalls wurde eine mögliche Beteiligung von Caspase-12 und eine ER-Streß vermittelte …
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Protektive in vitro Wirkung mitochondrialer Entkoppler auf die Apoptose in Leukämiezellinien
… Reduktion des intrazellulären CPP-32-Spiegels (Procaspase-3) zeigte sich bereits 6 Stunden nach Behandlungsbeginn mit FCCP, statt, verglichen mit 24 Stunden unter normalen Inkubationsbedingungen. Im Verlauf der durch FCCP induzierten Apoptose konnten wir mittels konventioneller …