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 13 of 13 for “"pentamidine"”.
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Analytical and metabolic studies of the trypanocidal diamidines
… failure. The metabolism of diminazene and pentamidine in isolated rat and pig hepatocytes have been investigated. Diminazene was not metabolized in either rat or pig hepatocytes. While there were no obvious qualitative differences in the metabolic profiles of pentamidine in either of the …
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Molecular mechanism of Trypanosoma brucei Aquaglyceroporin 2
… the uptake of two of the drugs used clinically, pentamidine and melarsoprol. TbAQP2 mutations or the formation of a chimeric gene with TbAQP3 (TbAQP2X3) cause pentamidine-melarsoprol cross-resistance (PMXR). TbAQP2 is an aquaporin, a type of water permeable pore forming integral membrane protein, …
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Factors influencing the spread and selection of drug resistance in Human African Trypanosomiasis
… the diamidine group of trypanocides, diminazene, pentamidine and furamidine (DB75) are principally mediated through the TbAT1/P2. In addition, pentamidine is taken up by two additional T. brucei transporters called High Affinity Pentamidine Transporter (HAPT1) and the Low Affinity Pentamidine …
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Computer-aided drug design and the biological evaluation of anti-cancer drugs
… that has a pivotal role in cancer survival and Pentamidine, an anti-parasitic drug that has recently been demonstrated to possess tumour-killing activity. A hierarchical methodology consisting of a similarity search followed by structure-based virtual screening of the ZINC database was …
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Blood-CNS transport mechanisms in pathophysiology and drug delivery
… agents to the brain. The anti-trypanosomal drug pentamidine was shown previously by our group to be a substrate for efflux from the blood-CNS barriers and does not ordinarily accumulate to pharmacologically relevant levels in the brain. Pluronic® copolymers are known biological response modifiers …
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New therapeutic strategies against trypanosomiasis and leishmaniasis
… compounds displayed EC50 values below that of pentamidine, the routinely used drug. Assessment of parasite growth pattern in the presence of choline analogues showed that two of the compounds, T1 and MS1, are fast acting, killing the population of BSF T. b. brucei within 8 h with the onset of …
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Synthetic strategies for potential trypanocides
… The sleeping sickness drugs melarsoprol and pentamidine contain P2 motifs. Compounds comprising a P2 targeting motif, a linker and a trypanocidal moiety were synthesized. Initially, a diaminotriazine P2 motif was attached to a trypanocidal tetrahydroquinoline (THQ) protein farnesyl …
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Structure-Function and Behavioral Studies on the Glutamate Delta-1 Receptor
… GluD1A654C, and GluD1F655A. Channel blockers pentamidine and NASP inhibited currents through the GluD1 mutant receptors. D-serine and extracellular calcium had opposing effects on GluD1 mutants and a chimeric GluD1-D2 lurcher. D-serine decreased currents through GluD1F655A and chimeric …
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Investigation towards the role of LmxOSM3.1 phosphorylation and the identification of its interaction partners using an improved method of proximity labelling
… amphotericin B, miltefosine, paromomycin, and pentamidine. Unfortunately, they do not come without limitations, hence, more effective treatments are needed. Kinases and kinesins have been shown to be promising drug targets.;LmxOSM3.1 is expected to be a plus end-directed 170kDa, homodimeric …
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Putative phosphodiesterase inhibitors as potential new chemotherapies against African Trypanosomiasis
… and some Series 1 compounds are on a par with pentamidine and melarsoprol. No major cross-resistance was displayed by the TbAT1 knockout strain to either Series 1 or the GJS series. Similarly, a panel of Series 1 compounds tested against the B48 strain (resistant to pentamidine and …
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Linkage mapping and genetic analysis of Trypanosoma brucei
… to sensitivity to the trypanocidal drug, pentamidine, for which phenotypic variation between the parents was characterised both in vitro and in vivo in this thesis. The ability of the T.brucei genetic maps to pinpoint loci underlying phenotypic variation is limited by the number of …
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Multidimensional liquid chromatographic separations for proteomics
… analyses. UV-absorbance maps of wild-type and pentamidine resistant Leishmania donovani were compared using standard two dimensional gel electrophoresis analysis software and resulted in the identification of a small number of quantitiative differences. Modifications to the isotope coded …
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Phytochemistry and biological studies of constituents from Breonadia Salicina (VAHL) Hepper and J. R. I. Wood
… On the other hand, the reference drug pentamidine showed an IC50 of 10.2 ± 0.07 μg/mL. The anti-oxidant assays revealed that the crude stem bark extract had the highest DPPH free radical scavenging activity, with an IC50 of 41.7263 ± 7.6401 μg/mL. Furthermore, the crude root extract had …