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 19 of 19 for “"chloroquine (CQ)"”.
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Malaria treatment seeking behaviour and access to artemisinin combination therapy : a case of Mushin, Lagos, Nigeria
… in Nigeria because of resistance of malaria to chloroquine (CQ) and sulphadoxine pyrimethamine (SP). However, very little is known about malaria and treatment-seeking patterns and the use of ACTs since the adoption of the treatment policy more than 6 years ago in Nigeria.
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Quercetin and chloroquine synergistically induces cell death in glioma cells via the increase of Ca2+ and ROS levels
… We show herein that quercetin, a flavonoid, and chloroquine (CQ), an antimalarial drug, synergistically induce caspase-mediated apoptosis in T98G cells. Combined treatment with quercetin and CQ accumulated poly-ubiquitinated proteins and activated unfolded protein response (UPR) in these cells. …
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Utilisation of efficient reactions to combine moeities exhibiting biological activity to produce novel anti-infectives against HIV and malaria
Chloroquine (CQ) was previously identified as a potential anti-HIV agent and reported to inhibit the production of infectious viral particles at concentrations which are non toxic to human cultured cells. It is speculated that this activity is associated with the decreased production of the heavily …
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Discovery of benzamides and triarylimidazoles active against Plasmodium falciparum via haemozoin inhibition : high throughput screening, synthesis and structure-activity relationships
… to be good inhibitors of βH relative to the chloroquine (CQ) and amodiaquine (AQ) controls. A further 171 compounds were found to inhibit parasite growth, showing improved hit rates from previous HTS efforts. Two scaffolds (A=benzamides and B=triarylimidazoles) were selected for further …
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Directed Evolution of Macrocyclic Peptides For Inhibition of Autophagy
… resistance and dormancy in many cancer types. Chloroquine (CQ) and hydroxychloroquine (HCQ), two autophagy inhibitors in clinical trials, suffer from poor pharmacokinetics and high toxicity at therapeutic dosages. This has prompted intense interest in the development of targeted autophagy …
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Overcoming chemoresistance in osteosarcoma: the role of autophagy in cell death or survival following chemotherapy
… results confirmed this pattern. Combination of chloroquine (CQ) with chemotherapy had a significant effect on OS cell proliferation and cell death rate. However, the results of CQ combination could not be attributed to autophagy inhibition, due to the substantial cytotoxic effects that was …
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Nutrient-dependent effects of the autophagy-lysosomal inhibitor, Chloroquine, on cell death and lysosomal functionality
… utilised the autophagy-lysosomal inhibitor Chloroquine (CQ) since this compound is currently in clinical trials for a variety of blood and solid cancers, including breast cancer. Here, the mechanisms of CQ and furthermore, the potential of combining this drug with metabolic targeting …
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The Role of Autophagy in the Pathogenesis and Clinical Course of Abdominal Aortic Aneurysms
… administration of the autophagy inhibitor chloroquine (CQ) did not alter the development, progression or rupture of AAA in mice. However, smooth muscle specific (SMC) ATG7 deficiency enhanced the susceptibility to AAA formation evident by the formation of pre-aneurysmal changes, emphasizing …
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Synthesis and SAR investigation of haemozoin-inhibiting quinazolines active against Plasmodium falciparum
… tested for biological antimalarial activities in chloroquine sensitive (NF54) and chloroquine resistant (DD2) parasites. Cytotoxicity was tested in Chinese Hamster Ovarian cells. Of the 21 synthesised quinazoline derivatives 15 were active with IC₅₀ values below 1500 μM for βHI and of the 15, ten …
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Therapeutic targeting of DGKA-mediated macropinocytosis in lymphangioleiomyomatosis
… upregulates pathways of extracellular nutrient acquisition. Macropinocytosis, a form of clathrin-independent endocytosis, is upregulated in TSC2-deficient cells. We performed a high-throughput compound screen utilizing a repurposing drug library. We identified that ritanserin, a diacylglycerol …
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Molecular Mechanisms of Itch Sensations
… i.d.) application of GRPR antagonists inhibits chloroquine: CQ), GRP and allergic contact dermatitis: ACD)-induced scratching responses in mice. It is interesting to find peripheral GRPR functions for itch sensation because it will provide an alternative therapeutic route for itch by targeting …
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Probing the protein homeostasis mechanisms in long-lived naked mole-rats
… of autophagy markers under rapamycin (RA) and chloroquine (CQ)-treated conditions were monitored in an NMR skin fibroblast cell line, where the sensitivity of the NMR skin fibroblasts to CQ, when compared to NMR kidney fibroblasts and mouse NIH3T3 embryonic cells, seemed to be partly attributed …
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Glutathione metabolism of Plasmodium falciparum
… involved in resistance to the antimalarial drug chloroquine (CQ). CQ was for a long time the first line antimalarial drug due to its high efficiency, low cost and low toxicity, but is now widely inefficient in the treatment of the disease. CQ resistance is associated with mutations in the CQ …
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Mechanistic study on the therapeutic strategy to enhance glioma cell death through inhibition of proteasome and lysosome
… Bortezomib (BZ), a proteasome inhibitor, and chloroquine (CQ), a lysosomotropic agent, can disrupt cellular protein homeostasis (proteostasis) via interruption of protein degradation systems, including proteasome and lysosome. In part I, we investigate the role of eIF2a in BZ-induced cell …
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Physicochemical, biological and β-haematin inhibiting activity of pyrido-dibemequines, pyrido[1,2-α]benzimidazoles and their derivatives
… formation probed. The pDBQs constitute reversed chloroquines with a 4-aminoquinoline nucleus hybridised to a dibenzylmethylamine side group that serves as a chemosensitising moiety. The pDBQ derivatives showed moderate to high solubility (52 - 197 μM) and permeability (LogPₐₚₚ: -4.6 - -3.6) at pH …
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Quantum dot labelled antimalarials and investigation of their interaction with synthetic haemozoin
Chloroquine (CQ) is a well-known antimalarial drug acting through the inhibition of the formation of haemozoin crystals in the Plasmodium parasite’s digestive vacuole within human infected red blood cells. The formation of haemozoin is considered a defence strategy of the parasite in order to …
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Determining the solubility of haematin and haem-drug complexes at relevant pH in aqueous medium via spectrophotometric titration
… methanols — represented in this study by chloroquine (CQ) and quinidine (QD), respectively — are widely accepted to act against the most virulent malaria parasite, Plasmodium falciparum, via the haemozoin inhibition pathway within the acidic digestive vacuole (DV) of the pathogen. However, …
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Probing the chemical biology involved in the haem detoxification pathway of the human malaria parasite, plasmodium falciparum
… crystals. Given that antimalarials like chloroquine (CQ), amodiaquine (AQ) and piperaquine (PPQ) target this process, the pathway has received tremendous recognition within the drug discovery and development arena as a valuable, druggable target. However, the pathway involves multiple …
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A pharmacokinetic and antimalarial efficacy evaluation of pyridodibemequines and their metabolites
… with the intention of reversing resistance in chloroquine-resistant (CQR) strains of Plasmodium falciparum. These hybrid molecules integrate a 4-amino-7-chloroquinoline antiplasmodial core with a modified dibenzylmethylamine side chain, which interacts with the CQR mutant P. falciparum …