FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2808753309> ?p ?o ?g. }

• W2808753309 endingPage "227" @default.
• W2808753309 startingPage "219" @default.
• W2808753309 abstract "Celecoxib was characterized as a substrate of human cytochrome P450 (CYP) 2D6 in vitro. In recombinant CYP2D6, celecoxib hydroxylation showed atypical substrate inhibition kinetics with apparent Km, Ki, and Vmax of 67.2 μM, 12.6 μM, and 1.33 μM/min, respectively. In human liver microsomes (HLMs), a concentration-dependent inhibition of celecoxib hydroxylation by quinidine was observed after CYP2C9 and CYP3A4 were inhibited. In individual HLMs with variable CYP2D6 activities, a significant correlation was observed between celecoxib hydroxylation and CYP2D6-selective dextromethorphan O-demethylation when CYP2C9 and CYP3A4 activities were suppressed (r = 0.97, P < 0.0001). Molecular modeling showed two predominant docking modes of celecoxib with CYP2D6, resulting in either a substrate or an inhibitor. A second allosteric binding antechamber, which stabilized the inhibition mode, was revealed. Modeling results were consistent with the observed substrate inhibition kinetics. Using HLMs from individual donors, the relative contribution of CYP2D6 to celecoxib metabolism was found to be highly variable and dependent on CYP2C9 genotypes, ranging from no contribution in extensive metabolizers with CYP2C9*1*1 genotype to approximately 30% in slow metabolizers with allelic variants CYP2C9*1*3 and CYP2C9*3*3. These results demonstrate that celecoxib may become a potential victim of CYP2D6-associated drug-drug interactions, particularly in individuals with reduced CYP2C9 activity." @default.
• W2808753309 created "2018-06-29" @default.
• W2808753309 creator A5019904448 @default.
• W2808753309 creator A5067010583 @default.
• W2808753309 creator A5077611406 @default.
• W2808753309 creator A5083889409 @default.
• W2808753309 date "2018-10-01" @default.
• W2808753309 modified "2023-10-11" @default.
• W2808753309 title "Celecoxib is a substrate of CYP2D6: Impact on celecoxib metabolism in individuals with CYP2C9*3 variants" @default.
• W2808753309 cites W1976056134 @default.
• W2808753309 cites W1987941468 @default.
• W2808753309 cites W2002173485 @default.
• W2808753309 cites W2008570013 @default.
• W2808753309 cites W2009313893 @default.
• W2808753309 cites W2011048896 @default.
• W2808753309 cites W2034008127 @default.
• W2808753309 cites W2050620617 @default.
• W2808753309 cites W2051165003 @default.
• W2808753309 cites W2061694980 @default.
• W2808753309 cites W2061799302 @default.
• W2808753309 cites W2064650404 @default.
• W2808753309 cites W2065462507 @default.
• W2808753309 cites W2070921940 @default.
• W2808753309 cites W2072180710 @default.
• W2808753309 cites W2082907683 @default.
• W2808753309 cites W2089353933 @default.
• W2808753309 cites W2105587896 @default.
• W2808753309 cites W2108136678 @default.
• W2808753309 cites W2138332753 @default.
• W2808753309 cites W2152354957 @default.
• W2808753309 cites W2163756514 @default.
• W2808753309 cites W2328207411 @default.
• W2808753309 doi "https://doi.org/10.1016/j.dmpk.2018.06.001" @default.
• W2808753309 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30219715" @default.
• W2808753309 hasPublicationYear "2018" @default.
• W2808753309 type Work @default.
• W2808753309 sameAs 2808753309 @default.
• W2808753309 citedByCount "17" @default.
• W2808753309 countsByYear W28087533092019 @default.
• W2808753309 countsByYear W28087533092020 @default.
• W2808753309 countsByYear W28087533092021 @default.
• W2808753309 countsByYear W28087533092022 @default.
• W2808753309 countsByYear W28087533092023 @default.
• W2808753309 crossrefType "journal-article" @default.
• W2808753309 hasAuthorship W2808753309A5019904448 @default.
• W2808753309 hasAuthorship W2808753309A5067010583 @default.
• W2808753309 hasAuthorship W2808753309A5077611406 @default.
• W2808753309 hasAuthorship W2808753309A5083889409 @default.
• W2808753309 hasConcept C109650736 @default.
• W2808753309 hasConcept C119795356 @default.
• W2808753309 hasConcept C181199279 @default.
• W2808753309 hasConcept C185592680 @default.
• W2808753309 hasConcept C2776467144 @default.
• W2808753309 hasConcept C2780339425 @default.
• W2808753309 hasConcept C2781109383 @default.
• W2808753309 hasConcept C2781245242 @default.
• W2808753309 hasConcept C33664856 @default.
• W2808753309 hasConcept C3946865 @default.
• W2808753309 hasConcept C526171541 @default.
• W2808753309 hasConcept C55493867 @default.
• W2808753309 hasConcept C62231903 @default.
• W2808753309 hasConcept C86803240 @default.
• W2808753309 hasConcept C87644729 @default.
• W2808753309 hasConcept C89311334 @default.
• W2808753309 hasConcept C98274493 @default.
• W2808753309 hasConceptScore W2808753309C109650736 @default.
• W2808753309 hasConceptScore W2808753309C119795356 @default.
• W2808753309 hasConceptScore W2808753309C181199279 @default.
• W2808753309 hasConceptScore W2808753309C185592680 @default.
• W2808753309 hasConceptScore W2808753309C2776467144 @default.
• W2808753309 hasConceptScore W2808753309C2780339425 @default.
• W2808753309 hasConceptScore W2808753309C2781109383 @default.
• W2808753309 hasConceptScore W2808753309C2781245242 @default.
• W2808753309 hasConceptScore W2808753309C33664856 @default.
• W2808753309 hasConceptScore W2808753309C3946865 @default.
• W2808753309 hasConceptScore W2808753309C526171541 @default.
• W2808753309 hasConceptScore W2808753309C55493867 @default.
• W2808753309 hasConceptScore W2808753309C62231903 @default.
• W2808753309 hasConceptScore W2808753309C86803240 @default.
• W2808753309 hasConceptScore W2808753309C87644729 @default.
• W2808753309 hasConceptScore W2808753309C89311334 @default.
• W2808753309 hasConceptScore W2808753309C98274493 @default.
• W2808753309 hasIssue "5" @default.
• W2808753309 hasLocation W28087533091 @default.
• W2808753309 hasLocation W28087533092 @default.
• W2808753309 hasOpenAccess W2808753309 @default.
• W2808753309 hasPrimaryLocation W28087533091 @default.
• W2808753309 hasRelatedWork W2023264313 @default.
• W2808753309 hasRelatedWork W2027148131 @default.
• W2808753309 hasRelatedWork W2043221233 @default.
• W2808753309 hasRelatedWork W2065675076 @default.
• W2808753309 hasRelatedWork W2077920591 @default.
• W2808753309 hasRelatedWork W2202139870 @default.
• W2808753309 hasRelatedWork W2980768026 @default.
• W2808753309 hasRelatedWork W3202891128 @default.
• W2808753309 hasRelatedWork W4207080932 @default.
• W2808753309 hasRelatedWork W4230554128 @default.
• W2808753309 hasVolume "33" @default.

• next