FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2073060384> ?p ?o ?g. }

• W2073060384 endingPage "717" @default.
• W2073060384 startingPage "703" @default.
• W2073060384 abstract "1. Artelinic acid (AL), a water-soluble artemisinin analogue for treatment of multidrug resistant malaria, is metabolized to the active metabolite dihydroqinghaosu (DQHS) solely by CYP3A4/5. Although AL is not metabolized by CYP2C9, it does inhibit diclofenac 4-hydroxylase activity with an IC50 = 115 muM. Interestingly, AL activates CYP2D6-mediated bufuralol metabolism in human liver microsomes but not recombinant CYP2D6-Val by ~30% at AL concentrations up to 100 muM. 2. In human liver microsomes, AL is metabolized to DQHS with a Km = 157 +/- 44 muM and Vmax = 0.77 +/- 0.56 nmol DQHS/min/mg protein. Human recombinant CYP3A4 catalysed the conversion of AL to DQHS with a Km = 102 +/- 23 muM and a Vmax = 1.96 +/- 0.38 nmol DQHS/min/nmol P450. The kinetic parameters (Km and Vmax) for DQHS formation from CYP3A5 were 189 +/- 19 muM and 3.60 +/= 0.42 nmol DQHS/min/nmol P450 respectively. 3. Inhibition studies suggest that azole antifungals and calcium channel blockers may present clinically significant drug-drug interactions. In human liver microsomes, ketoconazole and miconazole were potent competitive inhibitors of DQHS formation with a Ki = 0.028 and 0.124 muM respectively. Verapamil is a non-competitive inhibitor of DQHS formation in human liver microsomes with a Ki = 15muM." @default.
• W2073060384 created "2016-06-24" @default.
• W2073060384 creator A5006579028 @default.
• W2073060384 creator A5040346336 @default.
• W2073060384 creator A5058135075 @default.
• W2073060384 date "1999-01-01" @default.
• W2073060384 modified "2023-09-23" @default.
• W2073060384 title "Metabolism of artelinic acid to dihydroqinghaosu by human liver cytochrome P4503A" @default.
• W2073060384 cites W1748160049 @default.
• W2073060384 cites W1920717726 @default.
• W2073060384 cites W1951469402 @default.
• W2073060384 cites W1965031546 @default.
• W2073060384 cites W1980601413 @default.
• W2073060384 cites W1981972560 @default.
• W2073060384 cites W1991603747 @default.
• W2073060384 cites W1992822028 @default.
• W2073060384 cites W2006610890 @default.
• W2073060384 cites W2017504348 @default.
• W2073060384 cites W2017729229 @default.
• W2073060384 cites W2021519311 @default.
• W2073060384 cites W2044695596 @default.
• W2073060384 cites W2048796575 @default.
• W2073060384 cites W2049770869 @default.
• W2073060384 cites W2072494922 @default.
• W2073060384 cites W2083081513 @default.
• W2073060384 cites W2085283167 @default.
• W2073060384 cites W2090149382 @default.
• W2073060384 cites W2092116907 @default.
• W2073060384 cites W2098184601 @default.
• W2073060384 cites W2127623399 @default.
• W2073060384 cites W2792453324 @default.
• W2073060384 cites W4244827160 @default.
• W2073060384 doi "https://doi.org/10.1080/004982599238335" @default.
• W2073060384 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10456689" @default.
• W2073060384 hasPublicationYear "1999" @default.
• W2073060384 type Work @default.
• W2073060384 sameAs 2073060384 @default.
• W2073060384 citedByCount "32" @default.
• W2073060384 countsByYear W20730603842015 @default.
• W2073060384 countsByYear W20730603842016 @default.
• W2073060384 countsByYear W20730603842017 @default.
• W2073060384 countsByYear W20730603842020 @default.
• W2073060384 countsByYear W20730603842021 @default.
• W2073060384 countsByYear W20730603842022 @default.
• W2073060384 countsByYear W20730603842023 @default.
• W2073060384 crossrefType "journal-article" @default.
• W2073060384 hasAuthorship W2073060384A5006579028 @default.
• W2073060384 hasAuthorship W2073060384A5040346336 @default.
• W2073060384 hasAuthorship W2073060384A5058135075 @default.
• W2073060384 hasConcept C109650736 @default.
• W2073060384 hasConcept C150757390 @default.
• W2073060384 hasConcept C178790620 @default.
• W2073060384 hasConcept C181199279 @default.
• W2073060384 hasConcept C185592680 @default.
• W2073060384 hasConcept C202751555 @default.
• W2073060384 hasConcept C2777022698 @default.
• W2073060384 hasConcept C2777477808 @default.
• W2073060384 hasConcept C2777752497 @default.
• W2073060384 hasConcept C2779548794 @default.
• W2073060384 hasConcept C2780315139 @default.
• W2073060384 hasConcept C2781064554 @default.
• W2073060384 hasConcept C3946865 @default.
• W2073060384 hasConcept C519063684 @default.
• W2073060384 hasConcept C526171541 @default.
• W2073060384 hasConcept C55493867 @default.
• W2073060384 hasConcept C62231903 @default.
• W2073060384 hasConcept C86803240 @default.
• W2073060384 hasConcept C87644729 @default.
• W2073060384 hasConcept C89311334 @default.
• W2073060384 hasConcept C89423630 @default.
• W2073060384 hasConcept C98274493 @default.
• W2073060384 hasConceptScore W2073060384C109650736 @default.
• W2073060384 hasConceptScore W2073060384C150757390 @default.
• W2073060384 hasConceptScore W2073060384C178790620 @default.
• W2073060384 hasConceptScore W2073060384C181199279 @default.
• W2073060384 hasConceptScore W2073060384C185592680 @default.
• W2073060384 hasConceptScore W2073060384C202751555 @default.
• W2073060384 hasConceptScore W2073060384C2777022698 @default.
• W2073060384 hasConceptScore W2073060384C2777477808 @default.
• W2073060384 hasConceptScore W2073060384C2777752497 @default.
• W2073060384 hasConceptScore W2073060384C2779548794 @default.
• W2073060384 hasConceptScore W2073060384C2780315139 @default.
• W2073060384 hasConceptScore W2073060384C2781064554 @default.
• W2073060384 hasConceptScore W2073060384C3946865 @default.
• W2073060384 hasConceptScore W2073060384C519063684 @default.
• W2073060384 hasConceptScore W2073060384C526171541 @default.
• W2073060384 hasConceptScore W2073060384C55493867 @default.
• W2073060384 hasConceptScore W2073060384C62231903 @default.
• W2073060384 hasConceptScore W2073060384C86803240 @default.
• W2073060384 hasConceptScore W2073060384C87644729 @default.
• W2073060384 hasConceptScore W2073060384C89311334 @default.
• W2073060384 hasConceptScore W2073060384C89423630 @default.
• W2073060384 hasConceptScore W2073060384C98274493 @default.
• W2073060384 hasIssue "7" @default.
• W2073060384 hasLocation W20730603841 @default.
• W2073060384 hasOpenAccess W2073060384 @default.
• W2073060384 hasPrimaryLocation W20730603841 @default.
• W2073060384 hasRelatedWork W1972764254 @default.

• next