FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2101478629> ?p ?o ?g. }

• W2101478629 endingPage "1222" @default.
• W2101478629 startingPage "1217" @default.
• W2101478629 abstract "Both apicomplexan parasites Toxoplasma gondii and Plasmodium falciparum lack type I NADH dehydrogenases (complex I) but instead carry alternative (type II) NADH dehydrogenases, which are absent in mammalian cells and are thus considered promising antimicrobial drug targets. The quinolone-like compound 1-hydroxy-2-dodecyl-4(1H)quinolone (HDQ) was recently described as a high-affinity inhibitor of fungal alternative NADH dehydrogenases in enzymatic assays, probably by interfering with the ubiquinol binding site of the enzyme. We describe here that HDQ effectively inhibits the replication rates of P. falciparum and T. gondii in tissue culture. The 50% inhibitory concentration (IC50) of HDQ for T. gondii was determined to be 2.4+/-0.3 nM with a growth assay based on vacuole sizes and 3.7+/-1.4 nM with a growth assay based on beta-galactosidase activity. Quantification of the P. falciparum replication rate using a fluorometric assay revealed an IC50 of 14.0+/-1.9 nM. An important feature of the HDQ structure is the length of the alkyl side chain at position 2. Derivatives with alkyl side chains of C6, C8, C12 (HDQ), and C14 all displayed excellent anti-T. gondii activity, while a C5 derivative completely failed to inhibit parasite replication. A combined treatment of T. gondii-infected cells with HDQ and the antimalarial agent atovaquone, which blocks the ubiquinol oxidation site of cytochrome b in complex III, resulted in synergism, with a calculated fractional inhibitory concentration of 0.16 nM. Interference of the mitochondrial ubiquinone/ubiquinol cycle at two different locations thus appears to be a highly effective strategy for inhibiting parasite replication. HDQ and its derivatives, particularly in combination with atovaquone, represent promising compounds with a high potential for antimalarial and antitoxoplasmal therapy." @default.
• W2101478629 created "2016-06-24" @default.
• W2101478629 creator A5016479584 @default.
• W2101478629 creator A5036684937 @default.
• W2101478629 creator A5049218335 @default.
• W2101478629 creator A5058180554 @default.
• W2101478629 creator A5080350850 @default.
• W2101478629 date "2007-04-01" @default.
• W2101478629 modified "2023-09-27" @default.
• W2101478629 title "Growth Inhibition of <i>Toxoplasma gondii</i> and <i>Plasmodium falciparum</i> by Nanomolar Concentrations of 1-Hydroxy-2-Dodecyl-4(1 <i>H</i> )Quinolone, a High-Affinity Inhibitor of Alternative (Type II) NADH Dehydrogenases" @default.
• W2101478629 cites W1481682126 @default.
• W2101478629 cites W162317852 @default.
• W2101478629 cites W1969503178 @default.
• W2101478629 cites W1969932487 @default.
• W2101478629 cites W1977500078 @default.
• W2101478629 cites W1986111503 @default.
• W2101478629 cites W2011167792 @default.
• W2101478629 cites W2019851585 @default.
• W2101478629 cites W2020251171 @default.
• W2101478629 cites W2025605230 @default.
• W2101478629 cites W2029553134 @default.
• W2101478629 cites W2040519812 @default.
• W2101478629 cites W2053063939 @default.
• W2101478629 cites W2062733000 @default.
• W2101478629 cites W2063146761 @default.
• W2101478629 cites W2079099027 @default.
• W2101478629 cites W2088312274 @default.
• W2101478629 cites W2093244442 @default.
• W2101478629 cites W2108076979 @default.
• W2101478629 cites W2112191861 @default.
• W2101478629 cites W2115011002 @default.
• W2101478629 cites W2134610533 @default.
• W2101478629 cites W2138488546 @default.
• W2101478629 cites W2153629132 @default.
• W2101478629 cites W2156257778 @default.
• W2101478629 cites W2169100396 @default.
• W2101478629 cites W44681799 @default.
• W2101478629 doi "https://doi.org/10.1128/aac.00895-06" @default.
• W2101478629 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1855512" @default.
• W2101478629 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17242151" @default.
• W2101478629 hasPublicationYear "2007" @default.
• W2101478629 type Work @default.
• W2101478629 sameAs 2101478629 @default.
• W2101478629 citedByCount "83" @default.
• W2101478629 countsByYear W21014786292012 @default.
• W2101478629 countsByYear W21014786292013 @default.
• W2101478629 countsByYear W21014786292014 @default.
• W2101478629 countsByYear W21014786292015 @default.
• W2101478629 countsByYear W21014786292016 @default.
• W2101478629 countsByYear W21014786292017 @default.
• W2101478629 countsByYear W21014786292018 @default.
• W2101478629 countsByYear W21014786292019 @default.
• W2101478629 countsByYear W21014786292021 @default.
• W2101478629 countsByYear W21014786292022 @default.
• W2101478629 countsByYear W21014786292023 @default.
• W2101478629 crossrefType "journal-article" @default.
• W2101478629 hasAuthorship W2101478629A5016479584 @default.
• W2101478629 hasAuthorship W2101478629A5036684937 @default.
• W2101478629 hasAuthorship W2101478629A5049218335 @default.
• W2101478629 hasAuthorship W2101478629A5058180554 @default.
• W2101478629 hasAuthorship W2101478629A5080350850 @default.
• W2101478629 hasBestOaLocation W21014786291 @default.
• W2101478629 hasConcept C14471203 @default.
• W2101478629 hasConcept C159654299 @default.
• W2101478629 hasConcept C181199279 @default.
• W2101478629 hasConcept C185592680 @default.
• W2101478629 hasConcept C202751555 @default.
• W2101478629 hasConcept C203014093 @default.
• W2101478629 hasConcept C2777752497 @default.
• W2101478629 hasConcept C2778048844 @default.
• W2101478629 hasConcept C2778128430 @default.
• W2101478629 hasConcept C2778371730 @default.
• W2101478629 hasConcept C2778777121 @default.
• W2101478629 hasConcept C2779124865 @default.
• W2101478629 hasConcept C2779707156 @default.
• W2101478629 hasConcept C2779922871 @default.
• W2101478629 hasConcept C28859421 @default.
• W2101478629 hasConcept C29311851 @default.
• W2101478629 hasConcept C501593827 @default.
• W2101478629 hasConcept C55493867 @default.
• W2101478629 hasConcept C71240020 @default.
• W2101478629 hasConcept C86803240 @default.
• W2101478629 hasConceptScore W2101478629C14471203 @default.
• W2101478629 hasConceptScore W2101478629C159654299 @default.
• W2101478629 hasConceptScore W2101478629C181199279 @default.
• W2101478629 hasConceptScore W2101478629C185592680 @default.
• W2101478629 hasConceptScore W2101478629C202751555 @default.
• W2101478629 hasConceptScore W2101478629C203014093 @default.
• W2101478629 hasConceptScore W2101478629C2777752497 @default.
• W2101478629 hasConceptScore W2101478629C2778048844 @default.
• W2101478629 hasConceptScore W2101478629C2778128430 @default.
• W2101478629 hasConceptScore W2101478629C2778371730 @default.
• W2101478629 hasConceptScore W2101478629C2778777121 @default.
• W2101478629 hasConceptScore W2101478629C2779124865 @default.
• W2101478629 hasConceptScore W2101478629C2779707156 @default.
• W2101478629 hasConceptScore W2101478629C2779922871 @default.
• W2101478629 hasConceptScore W2101478629C28859421 @default.
• W2101478629 hasConceptScore W2101478629C29311851 @default.

• next