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 9 of 9 for “"Non-Mevalonate pathway"”.
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Inhibition of enzymes from the non-mevalonate pathway using fragment-based approaches
… against two essential target proteins in the non-mevalonate pathway (MEP), 1-deoxy-D-xylulose 5-phosphate synthase (DXS) from *D.radiodurans* and 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) from *E.coli*. There have been only a handful of reports of small molecules developed to …
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Investigating pathogen 4Fe-4S protein targets and cancer chemotherapies with bisphosphonate/diphosphate inhibitors
… of the Methyl Erythritol Phosphate (MEP; non-mevalonate pathway) pathway in bacterial and parasitic human pathogens and inhibition of isoprenoid synthases in human cancers. For the development of antibacterials and antiparasitics, this research investigates the structure, function, and …
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The design and synthesis of novel potential antimalarial compounds
… Each section covers a different biological pathway, its current importance as a potential drug target, and the syntheses towards a selection of natural products and analogues relevant to the pathway. In Section A, the novel approach towards a new class of n-formyl amides is described. …
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Mechanism, inhibition and spectroscopy of isoprenoid biosynthesis enzymes
… inhibition of several enzymes in two important pathways for isoprenoid biosynthesis. The first pair of enzyme are IspG and IspH, which constitute the last two steps in the MEP/DOXP (or non-mevalonate) pathway, which some bacteria, protozoa and plants rely on to produce the basic building blocks …
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Mechanisms of action and inhibition of [4Fe-4S] proteins IspG and IspH in isoprenoid biosynthesis
The methylerythritol phosphate pathway (also known as the non-mevalonate pathway) of isoprenoid biosynthesis is potentially an important anti-bacterial and anti-malarial drug target. However, the catalytic mechanisms of the last two enzymes in this pathway, IspG (also known as GcpE) and IspH (also …
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Toward the synthesis and evaluation of novel N-acylated FR-900098 analogs
… Plasmodium for isoprenoid biosynthesis via the non-mevalonate pathway, which does not exist in humans. Although FR-900098 was determined to be about twice as potent as fosmidomycin, it is important to note that, as a Streptomycete secondary metabolite, it is by no means optimized as a human …
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MMV008138 and analogs: potential novel antimalarial agents for P. falciparum
… and dimethylallyl pyrophosphate (DMAPP), via a non-mevalonate pathway: the methylerythritol phosphate (MEP) pathway. This pathway is not utilized by humans. Thus, compounds that target the MEP pathway and disrupt isoprenoid biosynthesis in P. falciparum hold promise as potent and safe new …
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Molecular target identification of antimalarial drugs using proteomic and metabolomic approaches
… through the methylerythritol phosphate (MEP) pathway in the malaria parasite while humans utilize the mevalonate pathway. Therefore, the MEP pathway is a source of drug targets for drug development. Our group has identified MMV008138 as anti-apicoplast inhibitor through phenotypic screening. …
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SYNTHESIS AND EVALUATION OF FOSMIDOMYCIN ANALOGUES AS ANTIMALARIAL AGENTS
… (DXR), which is involved in the DOXP pathway for isoprenoid synthesis, was chosen as drug target. This non-mevalonate pathway is not operating in humans and inhibitors of DXR can therefore be considered as selective for parasites. Fosmidomycin and its methyl homologue FR900098, …