Matches in SemOpenAlex for { <https://semopenalex.org/work/W23754229> ?p ?o ?g. }
Showing items 1 to 77 of
77
with 100 items per page.
- W23754229 abstract "Schering 66712 (5-fluoro-2-[4-[(2-phenyl-1H-imidazol5-yl)methyl]-1-piperzainyl]pyrimidine) is a mechanism-based inactivator of human cytochrome P450 2D6 (P450 2D6) that displays Type I binding with KS of 0.39 ± 0.10 μM. The partition ratio is approximately 300. Inactivation was not prevented by addition of an exogenous nucleophiles including potassium cyanide. Within 15 minutes of incubation with Schering 66712 and NADPH, ~100% of P450 2D6 activity was lost with ~40% loss in ability to binding CO. These findings support inactivation primarily by adduction of protein. ESI-LC-MS analysis of whole protein also indicates the presence of a protein adduct. Modeling of Schering 66712 in the active site of P450 2D6 suggests interaction between the phenyl group of Schering 66712 and the heme iron. (Supported by: NIH GM086767-01 and RGM086767Z, a grant from the Howard Hughes Medical Institute to Kalamazoo College, and the Hutchcroft Fund of Kalamazoo College)." @default.
- W23754229 created "2016-06-24" @default.
- W23754229 creator A5000683957 @default.
- W23754229 creator A5004392984 @default.
- W23754229 creator A5004490066 @default.
- W23754229 creator A5040361202 @default.
- W23754229 creator A5050737001 @default.
- W23754229 creator A5058389506 @default.
- W23754229 creator A5084420823 @default.
- W23754229 creator A5090586935 @default.
- W23754229 date "2010-04-01" @default.
- W23754229 modified "2023-10-13" @default.
- W23754229 title "Mechanism‐Based Inhibition of Human Cytochrome P450 2D6 by Schering 66712" @default.
- W23754229 doi "https://doi.org/10.1096/fasebj.24.1_supplement.512.3" @default.
- W23754229 hasPublicationYear "2010" @default.
- W23754229 type Work @default.
- W23754229 sameAs 23754229 @default.
- W23754229 citedByCount "0" @default.
- W23754229 crossrefType "journal-article" @default.
- W23754229 hasAuthorship W23754229A5000683957 @default.
- W23754229 hasAuthorship W23754229A5004392984 @default.
- W23754229 hasAuthorship W23754229A5004490066 @default.
- W23754229 hasAuthorship W23754229A5040361202 @default.
- W23754229 hasAuthorship W23754229A5050737001 @default.
- W23754229 hasAuthorship W23754229A5058389506 @default.
- W23754229 hasAuthorship W23754229A5084420823 @default.
- W23754229 hasAuthorship W23754229A5090586935 @default.
- W23754229 hasConcept C121332964 @default.
- W23754229 hasConcept C181199279 @default.
- W23754229 hasConcept C185592680 @default.
- W23754229 hasConcept C33664856 @default.
- W23754229 hasConcept C526171541 @default.
- W23754229 hasConcept C55493867 @default.
- W23754229 hasConcept C62520636 @default.
- W23754229 hasConcept C71924100 @default.
- W23754229 hasConcept C89611455 @default.
- W23754229 hasConcept C98274493 @default.
- W23754229 hasConceptScore W23754229C121332964 @default.
- W23754229 hasConceptScore W23754229C181199279 @default.
- W23754229 hasConceptScore W23754229C185592680 @default.
- W23754229 hasConceptScore W23754229C33664856 @default.
- W23754229 hasConceptScore W23754229C526171541 @default.
- W23754229 hasConceptScore W23754229C55493867 @default.
- W23754229 hasConceptScore W23754229C62520636 @default.
- W23754229 hasConceptScore W23754229C71924100 @default.
- W23754229 hasConceptScore W23754229C89611455 @default.
- W23754229 hasConceptScore W23754229C98274493 @default.
- W23754229 hasFunder F4320332161 @default.
- W23754229 hasIssue "S1" @default.
- W23754229 hasLocation W237542291 @default.
- W23754229 hasOpenAccess W23754229 @default.
- W23754229 hasPrimaryLocation W237542291 @default.
- W23754229 hasRelatedWork W1488739710 @default.
- W23754229 hasRelatedWork W1501688570 @default.
- W23754229 hasRelatedWork W1508366269 @default.
- W23754229 hasRelatedWork W1607090140 @default.
- W23754229 hasRelatedWork W172435491 @default.
- W23754229 hasRelatedWork W1781030166 @default.
- W23754229 hasRelatedWork W1963935092 @default.
- W23754229 hasRelatedWork W2002846063 @default.
- W23754229 hasRelatedWork W2004208423 @default.
- W23754229 hasRelatedWork W2018873107 @default.
- W23754229 hasRelatedWork W2366610611 @default.
- W23754229 hasRelatedWork W2912021585 @default.
- W23754229 hasRelatedWork W2953347784 @default.
- W23754229 hasRelatedWork W2977226855 @default.
- W23754229 hasRelatedWork W2977681485 @default.
- W23754229 hasRelatedWork W2999686842 @default.
- W23754229 hasRelatedWork W3021644605 @default.
- W23754229 hasRelatedWork W67776894 @default.
- W23754229 hasRelatedWork W2839007797 @default.
- W23754229 hasRelatedWork W2908146833 @default.
- W23754229 hasVolume "24" @default.
- W23754229 isParatext "false" @default.
- W23754229 isRetracted "false" @default.
- W23754229 magId "23754229" @default.
- W23754229 workType "article" @default.