FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2119441418> ?p ?o ?g. }

• W2119441418 endingPage "61" @default.
• W2119441418 startingPage "552" @default.
• W2119441418 abstract "Both ritonavir and indinavir were readily metabolized by human intestinal microsomes. Comparison of the patterns of metabolites in incubations with enterocyte microsomes and expressed cytochrome P450 (CYP) isozymes and immunoinhibition and chemical inhibition studies showed the essential role of the CYP3A subfamily in the metabolism of both protease inhibitors by the small intestine. Ritonavir was similarly biotransformed by microsomes containing expressed CYP3A4 or CYP3A5 isozymes (KM = 0.05-0.07 microM, Vmax = 1-1.4 nmol/min/nmol CYP). In contrast, both the patterns of metabolites and the enzyme kinetic parameters for the metabolism of indinavir by expressed CYP3A5 (KM = 0.21 microM, Vmax = 0.24 nmol/min/nmol CYP) and CYP3A4 (KM = 0.04 microM, Vmax = 0.68 nmol/min/nmol CYP) were different. The biotransformation of both indinavir and ritonavir in human enterocyte microsomes was characterized by very low KM values (0.2-0.4 microM for indinavir and <0.1 microM for ritonavir). The Vmax for indinavir metabolism was greater in enterocyte (163 +/- 35 pmol/min/mg protein) than in liver (68 +/- 44 pmol/min/mg protein) microsomes. The metabolism of ritonavir in liver and enterocyte microsomes was associated with inactivation of CYP3A. The initial Vmax for ritonavir metabolism by enterocyte microsomes was 89 +/- 59 pmol/min/mg protein. The apparent inactivation rate constants for intestinal CYP3A and expressed CYP3A4 were 0.078 and 0.135 min-1, respectively. Metabolic inactivation of CYP3A by ritonavir explains the improved bioavailability and pharmacokinetics of ritonavir and the sustained elevation of blood levels of other, concomitantly administered, substrates of CYP3A." @default.
• W2119441418 created "2016-06-24" @default.
• W2119441418 creator A5000833013 @default.
• W2119441418 creator A5003757116 @default.
• W2119441418 creator A5009590404 @default.
• W2119441418 creator A5021875515 @default.
• W2119441418 creator A5031597854 @default.
• W2119441418 creator A5043268325 @default.
• W2119441418 creator A5043364254 @default.
• W2119441418 creator A5085666941 @default.
• W2119441418 creator A5088023410 @default.
• W2119441418 date "1998-06-01" @default.
• W2119441418 modified "2023-10-18" @default.
• W2119441418 title "Metabolism of the human immunodeficiency virus protease inhibitors indinavir and ritonavir by human intestinal microsomes and expressed cytochrome P4503A4/3A5: mechanism-based inactivation of cytochrome P4503A by ritonavir." @default.
• W2119441418 cites W1493111652 @default.
• W2119441418 cites W160491367 @default.
• W2119441418 cites W1774961775 @default.
• W2119441418 cites W1775749144 @default.
• W2119441418 cites W1829225133 @default.
• W2119441418 cites W1856418608 @default.
• W2119441418 cites W1861468507 @default.
• W2119441418 cites W1896473479 @default.
• W2119441418 cites W1960832302 @default.
• W2119441418 cites W2005545399 @default.
• W2119441418 cites W2054728806 @default.
• W2119441418 cites W2056455169 @default.
• W2119441418 cites W2059588998 @default.
• W2119441418 cites W2060952336 @default.
• W2119441418 cites W2064799851 @default.
• W2119441418 cites W2070177020 @default.
• W2119441418 cites W2073965718 @default.
• W2119441418 cites W2087709871 @default.
• W2119441418 cites W2107567029 @default.
• W2119441418 cites W2109604183 @default.
• W2119441418 cites W2115641665 @default.
• W2119441418 cites W2115837402 @default.
• W2119441418 cites W2121690400 @default.
• W2119441418 cites W2130082288 @default.
• W2119441418 cites W2132185205 @default.
• W2119441418 cites W2143907788 @default.
• W2119441418 cites W2153490352 @default.
• W2119441418 cites W2154638204 @default.
• W2119441418 cites W2165781594 @default.
• W2119441418 cites W2169290209 @default.
• W2119441418 cites W2262017276 @default.
• W2119441418 cites W2268040487 @default.
• W2119441418 cites W2271167817 @default.
• W2119441418 cites W2273442981 @default.
• W2119441418 cites W2529334616 @default.
• W2119441418 cites W2099656602 @default.
• W2119441418 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9616191" @default.
• W2119441418 hasPublicationYear "1998" @default.
• W2119441418 type Work @default.
• W2119441418 sameAs 2119441418 @default.
• W2119441418 citedByCount "74" @default.
• W2119441418 countsByYear W21194414182012 @default.
• W2119441418 countsByYear W21194414182014 @default.
• W2119441418 countsByYear W21194414182015 @default.
• W2119441418 countsByYear W21194414182016 @default.
• W2119441418 countsByYear W21194414182017 @default.
• W2119441418 countsByYear W21194414182019 @default.
• W2119441418 countsByYear W21194414182021 @default.
• W2119441418 countsByYear W21194414182022 @default.
• W2119441418 countsByYear W21194414182023 @default.
• W2119441418 crossrefType "journal-article" @default.
• W2119441418 hasAuthorship W2119441418A5000833013 @default.
• W2119441418 hasAuthorship W2119441418A5003757116 @default.
• W2119441418 hasAuthorship W2119441418A5009590404 @default.
• W2119441418 hasAuthorship W2119441418A5021875515 @default.
• W2119441418 hasAuthorship W2119441418A5031597854 @default.
• W2119441418 hasAuthorship W2119441418A5043268325 @default.
• W2119441418 hasAuthorship W2119441418A5043364254 @default.
• W2119441418 hasAuthorship W2119441418A5085666941 @default.
• W2119441418 hasAuthorship W2119441418A5088023410 @default.
• W2119441418 hasConcept C109650736 @default.
• W2119441418 hasConcept C11824378 @default.
• W2119441418 hasConcept C142462285 @default.
• W2119441418 hasConcept C159047783 @default.
• W2119441418 hasConcept C181199279 @default.
• W2119441418 hasConcept C185592680 @default.
• W2119441418 hasConcept C203014093 @default.
• W2119441418 hasConcept C2522874641 @default.
• W2119441418 hasConcept C2776452011 @default.
• W2119441418 hasConcept C2777210460 @default.
• W2119441418 hasConcept C2777882243 @default.
• W2119441418 hasConcept C2779298103 @default.
• W2119441418 hasConcept C2779604457 @default.
• W2119441418 hasConcept C2780727368 @default.
• W2119441418 hasConcept C2993143319 @default.
• W2119441418 hasConcept C3013748606 @default.
• W2119441418 hasConcept C526171541 @default.
• W2119441418 hasConcept C55493867 @default.
• W2119441418 hasConcept C62231903 @default.
• W2119441418 hasConcept C86803240 @default.
• W2119441418 hasConcept C87644729 @default.
• W2119441418 hasConceptScore W2119441418C109650736 @default.
• W2119441418 hasConceptScore W2119441418C11824378 @default.
• W2119441418 hasConceptScore W2119441418C142462285 @default.

• next