FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2002173485> ?p ?o ?g. }

• W2002173485 endingPage "1253" @default.
• W2002173485 startingPage "1245" @default.
• W2002173485 abstract "Human cytochrome P450 (P450) 2D6 is an important enzyme involved in the metabolism of drugs, many of which are amines or contain other basic nitrogen atoms. Asp301 has generally been considered to be involved in electrostatic docking with the basic substrates, on the basis of previous modeling studies and site-directed mutagenesis. Substitution of Glu216 with a residue other than Asp strongly attenuated the binding of quinidine, bufuralol, and several other P450 2D6 ligands. Catalytic activity with the substrates bufuralol and 4-methoxyphenethylamine was strongly inhibited by neutral or basic mutations at Glu216 (>95%), to the same extent as the substitution of Asn at Asp301. Unlike the Asp301 mutants, the Gln216 mutant (E216Q) retained 40% enzyme efficiency with the substrate spirosulfonamide, devoid of basic nitrogen, suggesting that the substitutions at Glu216 affect binding of amine substrates more than other catalytic steps. Attempts to induce catalytic specificity toward new substrates by substitutions at Asp301 and Glu216 were unsuccessful. Collectively, the results provide evidence for electrostatic interaction of amine substrates with Glu216, and we propose that both of these acidic residues plus at least another residue(s) is (are) involved in binding the repertoire of P450 2D6 ligands." @default.
• W2002173485 created "2016-06-24" @default.
• W2002173485 creator A5015815568 @default.
• W2002173485 creator A5017888348 @default.
• W2002173485 creator A5058389506 @default.
• W2002173485 creator A5088708740 @default.
• W2002173485 date "2003-01-17" @default.
• W2002173485 modified "2023-10-10" @default.
• W2002173485 title "Role of Glutamic Acid 216 in Cytochrome P450 2D6 Substrate Binding and Catalysis" @default.
• W2002173485 cites W1509690851 @default.
• W2002173485 cites W1529636312 @default.
• W2002173485 cites W1532212858 @default.
• W2002173485 cites W1544140936 @default.
• W2002173485 cites W1603225698 @default.
• W2002173485 cites W1963761471 @default.
• W2002173485 cites W1969215912 @default.
• W2002173485 cites W1974876872 @default.
• W2002173485 cites W1984850614 @default.
• W2002173485 cites W1989363569 @default.
• W2002173485 cites W2011048896 @default.
• W2002173485 cites W2011565603 @default.
• W2002173485 cites W2039249350 @default.
• W2002173485 cites W2042738756 @default.
• W2002173485 cites W2055143705 @default.
• W2002173485 cites W2090991101 @default.
• W2002173485 cites W2131414900 @default.
• W2002173485 cites W2156693191 @default.
• W2002173485 cites W2159529011 @default.
• W2002173485 cites W2228413566 @default.
• W2002173485 cites W4236830009 @default.
• W2002173485 cites W4252282252 @default.
• W2002173485 doi "https://doi.org/10.1021/bi027085w" @default.
• W2002173485 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12564927" @default.
• W2002173485 hasPublicationYear "2003" @default.
• W2002173485 type Work @default.
• W2002173485 sameAs 2002173485 @default.
• W2002173485 citedByCount "54" @default.
• W2002173485 countsByYear W20021734852012 @default.
• W2002173485 countsByYear W20021734852013 @default.
• W2002173485 countsByYear W20021734852014 @default.
• W2002173485 countsByYear W20021734852015 @default.
• W2002173485 countsByYear W20021734852016 @default.
• W2002173485 countsByYear W20021734852017 @default.
• W2002173485 countsByYear W20021734852018 @default.
• W2002173485 countsByYear W20021734852020 @default.
• W2002173485 countsByYear W20021734852021 @default.
• W2002173485 countsByYear W20021734852022 @default.
• W2002173485 crossrefType "journal-article" @default.
• W2002173485 hasAuthorship W2002173485A5015815568 @default.
• W2002173485 hasAuthorship W2002173485A5017888348 @default.
• W2002173485 hasAuthorship W2002173485A5058389506 @default.
• W2002173485 hasAuthorship W2002173485A5088708740 @default.
• W2002173485 hasConcept C103408237 @default.
• W2002173485 hasConcept C104317684 @default.
• W2002173485 hasConcept C107824862 @default.
• W2002173485 hasConcept C131779359 @default.
• W2002173485 hasConcept C143065580 @default.
• W2002173485 hasConcept C159110408 @default.
• W2002173485 hasConcept C161790260 @default.
• W2002173485 hasConcept C16318435 @default.
• W2002173485 hasConcept C178790620 @default.
• W2002173485 hasConcept C181199279 @default.
• W2002173485 hasConcept C185592680 @default.
• W2002173485 hasConcept C2781338088 @default.
• W2002173485 hasConcept C41183919 @default.
• W2002173485 hasConcept C41685203 @default.
• W2002173485 hasConcept C526171541 @default.
• W2002173485 hasConcept C55493867 @default.
• W2002173485 hasConcept C71240020 @default.
• W2002173485 hasConcept C71924100 @default.
• W2002173485 hasConceptScore W2002173485C103408237 @default.
• W2002173485 hasConceptScore W2002173485C104317684 @default.
• W2002173485 hasConceptScore W2002173485C107824862 @default.
• W2002173485 hasConceptScore W2002173485C131779359 @default.
• W2002173485 hasConceptScore W2002173485C143065580 @default.
• W2002173485 hasConceptScore W2002173485C159110408 @default.
• W2002173485 hasConceptScore W2002173485C161790260 @default.
• W2002173485 hasConceptScore W2002173485C16318435 @default.
• W2002173485 hasConceptScore W2002173485C178790620 @default.
• W2002173485 hasConceptScore W2002173485C181199279 @default.
• W2002173485 hasConceptScore W2002173485C185592680 @default.
• W2002173485 hasConceptScore W2002173485C2781338088 @default.
• W2002173485 hasConceptScore W2002173485C41183919 @default.
• W2002173485 hasConceptScore W2002173485C41685203 @default.
• W2002173485 hasConceptScore W2002173485C526171541 @default.
• W2002173485 hasConceptScore W2002173485C55493867 @default.
• W2002173485 hasConceptScore W2002173485C71240020 @default.
• W2002173485 hasConceptScore W2002173485C71924100 @default.
• W2002173485 hasIssue "5" @default.
• W2002173485 hasLocation W20021734851 @default.
• W2002173485 hasLocation W20021734852 @default.
• W2002173485 hasOpenAccess W2002173485 @default.
• W2002173485 hasPrimaryLocation W20021734851 @default.
• W2002173485 hasRelatedWork W2004834660 @default.
• W2002173485 hasRelatedWork W2024647076 @default.
• W2002173485 hasRelatedWork W2040122145 @default.
• W2002173485 hasRelatedWork W2349738535 @default.
• W2002173485 hasRelatedWork W2358175167 @default.

• next