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 7 of 7 for “"Emetine"”.
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Studies on some dehydrogenation products of emetine
… product obtained by mild oxidation of emetine. The primary aim was to obtain information about some of the dehydrogenation products of emetine which would permit elucidation of their structures. Attempts to prepare new disasteroisomers of emetine by reduction of the unsaturated …
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Lead optimisation of dehydroemetine as an antimalarial option through drug repositioning and molecular modelling
… the previously widely-used anti-amoebic drug emetine dihydrochloride as a potent inhibitor of Plasmodium falciparum K1 strain parasites (IC50: 47 + 2.17 nM). Emetine is not currently in use due to its emetic and cardiotoxic effects.The cryo-EM structure (3J7A) depicting the emetine binding …
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Accelerating antimalarial drug discovery through repositioning
… of the hits. From these, antiamoebic compound emetine dihydrochloride hydrate was identified as a potent inhibitor of the multidrug resistant Plasmodium falciparum, strain K1, with an IC50 of 47 nM (95 %confidence interval 44.92-49.17). Further characterisation of the compound involved analysis …
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Development of novel strategies to combat multidrug resistance mediated by efflux transporters and intracellular bacteria
… rapidly synthesize a library of dimers based on emetine and quinine. This resulted in triazole bearing dimers that potently inhibited P-gp efflux. Bivalent quinine probes were also developed as potential mechanistic probes of P-gp. Further, the bivalent strategy was expanded to the antimalarial …
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Using Cell Painting and Chemical Data for Small-molecule Bioactivity and Toxicity Prediction
… including dual-acting compounds such as emetine. This approach therefore offers a biologically relevant way to interpret the cell morphological features derived using software such as CellProfiler and to generate hypotheses for experimental validation. In summary, our work demonstrates …
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Re-evaluation of the hypothesis that LTP has two temporal phases and that the late phase is protein synthesis-dependent
… However, long-lasting pretreatment with the PSI emetine blocked LTP by LTP-unrelated mechanism as the drug showed deteriorating effect on the baseline response. In contrast, depleting the protein repertoire in the slice by long-lasting pretreatment with the PSI cycloheximide deteriorated the …
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Interrogating novel functions of the I kappa B kinases via CRISPR-Cas9 gene editing and small molecule inhibition
… meanwhile, exhibited wild-type NEMO expression. Emetine-chase and radioactive pulse chase labelling experiments demonstrated that the half-life of NEMO in IKKα and IKKα/β DKO cells was significantly shortened due to enhanced proteasomal turnover. Bioinformatics analyses predicted significant …