
NCBI . NLM . NIH . GOV {
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Title[redir]:
Comparative folate metabolism in humans and malaria parasites (part I): pointers for malaria treatment from cancer chemotherapy - PMC
Description:
New inhibitors are urgently needed to overcome the burgeoning problem of drug resistance in the treatment of Plasmodium falciparum infection. Targeting the folate pathway has proved to be a powerful strategy for drug development against rapidly ...
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Keywords {🔍}
doi, folate, google, scholar, pubmed, falciparum, plasmodium, parasite, enzymes, malaria, drug, enzyme, cells, synthesis, chthf, inhibitors, dhfr, pmc, targets, pathway, synthase, article, mammalian, figure, metabolism, agents, antimalarial, target, reaction, development, clinical, chothf, free, parasitol, cancer, human, fds, methionine, dihydrofolate, reactions, activities, bifunctional, treatment, serine, protein, novo, shmt, analogs, parasites, resistance,
Topics {✒️}
folypoly-γ-glutamate synthetase substrates folylpoly-γ-glutamate specificity free γ-glutamyl moiety 5′-phosphoribosyl-5-amino-4-imidazolecarboxamide formyltransferase mgatp-dependent sequential attachment ccrf-cem cell lines extremely long half-life dhfr-inhibiting diaminotriazine antimalarials dihydrofolate reductase–thymidylate synthase cobalamin-dependent methionine synthase nadp-dependent trifunctional protein γ-glutamyl peptide bonds pmc beta search preliminary x-ray analysis shorter-acting chlorproguanil/dapsone bifunctional methylenetetrahydrofolate dehydrogenase/cyclohydrolase bifunctional dehydrogenase–cyclohydrolase enzymes glycine-cleavage enzyme system understanding structure–function relationships potent diaminotriazine-based inhibitors de novo thymidylate synthesize de novo similar considerations apply anti-ts folate analogs anti-ts antimalarial drug major folate-based reactions develop anti-ts agents short-acting formulation enable sufficient specificity de novo pathway potent anti-dhfr agents cell cycle effects treat sp-resistant parasites de novo synthesis c1-thf synthase publisher site pdf thymidylate synthase inhibitors anti-ts compounds tested x-ray structure [45] γ-glutamyl hydrolase high-affinity metabolites experimental stage target mutant dihydrofolate reductases rapidly multiplying systems quinazoline antifolate directed united states government 5-methyl derivative amethopterin poor pharmacokinetic properties longer retention times producing sufficient amounts
Questions {❓}
- Cobalamin-dependent methionine synthase and serine hydroxymethyltransferase: targets for chemotherapeutic intervention?
- Pyrimethamine–sulfadoxine resistance in Plasmodium falciparum: what next?
- What do folate derivatives do?
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