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 14 of 14 for “"PAC-1"”.
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Development of PAC-1 as a privileged agent for combination chemotherapy
… across many diverse cancer types. PAC-1 is a small-molecule that facilitates procaspase-3 activation by relieving physiological zinc- mediated inhibition of auto-proteolytic activation. Activation of procaspase-3 by PAC-1 was previously demonstrated to induce apoptosis in cancer …
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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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Identifying the basis for anticancer synergy with PAC-1, with applications to meningioma
Submission published under a 24 month embargo labeled 'Closed Access', the embargo will last until 2024-12-01
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Evaluation of therapy for canine intracranial neoplasia using PAC-1, a novel and potent procaspase-3 activator
… resection and limiting therapeutic options. PAC-1 is a novel, blood-brain barrier penetrant, 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 …
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The discovery and characterization of anticancer procaspase activating compounds
… anticancer application of procaspase activators PAC-1 and S-PAC-1, the identification of novel procaspase activating compounds, and the evaluation of procaspase-3 levels in human cancers. Several procaspase activating compounds have been discovered in the Hergenrother laboratory through …
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Procaspase-3 activation as a strategy to overcome resistance to targeted anticancer therapies
… procaspase-3 activating small molecule (PAC-1) as an anticancer therapy. Activation of an executioner caspase such as caspase-3 leads to cleavage of hundreds of proteins in the cell, leading eventually to apoptotic cell death. In Chapter 2, I will first discuss the proteomic …
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The Modulation of Life and Death: Small Molecule Activators and Inhibitors of Necrotic and Apoptotic Pathways
… a small molecule activator of procaspase-3 (PAC-1) and an inhibitor of PARG (PIP-1) were identified. PAC-1 was shown to potently induce apoptosis in mammalian cells in a manner directly proportional to the amount of procaspase-3 contained within those cells. As all normal cells contain …
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Investigating procaspase-3 as a potential therapeutic target in canine osteosarcoma
… cancer cells. This work 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. …
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Small molecule activators of procaspase-3 as an anticancer strategy
… first small molecule activator of procaspase-3 (PAC-1) was reported by the Hergenrother laboratory. The studies described herein build on that discovery to expand our understanding of the potential and promise of small molecule activators of procaspase-3 in the treatment of cancer. …
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Small Molecule Modulation of Caspase Enzymatic Activity
… 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, the most physiologically …
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Investigating couplet strategies incorporating 4 pillars of cancer therapy
… 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 chemotherapeutics, which has …
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Investigating Apoptosis Pathway In Chronic Lymphocytic Leukemia: Stromal Influence and Therapeutic Activation
… Our studies with L14R8, a second generation PAC-1 analog [Procaspase activating compound-1 (PAC-1; Vanquish Oncology)] revealed that L14R8-induced cell death was specific to CLL cells and was independent of prognostic markers and microenvironmental factors. Mechanistically, L14R8 acted …
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An investigation of the role of ACTN1 in platelet formation and of platelet function in myeloma
… protein but mutations have a tissue-specific impact, causing CMTP, characterised by low platelet count and large platelet size. It was previously shown that mutations in the actin-binding domain of actinin-1 increase the affinity of actinin-1 for actin filaments. In this study, nine mutations in …
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CHCHD2 and the tumor microenvironment in glioblastoma
… obstacle to more effective therapies is the impact of the surrounding tumor microenvironment on intracellular signaling, which has the potential to undermine targeted treatments and advance tumor malignancy, progression, and resistance to therapy. Additionally, mitochondria, generally regarded …