Matches in SemOpenAlex for { <https://semopenalex.org/work/W3166335487> ?p ?o ?g. }
Showing items 1 to 77 of
77
with 100 items per page.
- W3166335487 abstract "Cytochromes P450 (CYPs) are a superfamily of human enzymes essential for the metabolism of drugs, xenobiotics, and many endogenous hormones such as steroids. In adults, CYP3A4 is the primary xenobiotic metabolizing enzyme expressed in the liver and intestine, and its metabolism of xenobiotics has been extensively studied over the past several decades. In contrast, CYP3A7, the 3A sub-family enzyme predominantly expressed in neonates and developing infants, has been less studied and has no standard or efficient high-throughput screening (HTS) method to determine its enzymatic activity. As more pharmaceutical agents are being developed to specifically target this fragile patient population, a robust and reliable HTS assay is needed in order to facilitate pre-clinical testing of drug candidates for both safety and efficacy. Additionally, development of such an assay would be extremely beneficial to identify potential drug-drug interactions that might occur before actual administration of the drugs. In this study, our goal was to identify an efficient, cost-effective fluorescent substrate specific for CYP3A7 and develop an HTS assay supporting it. To that end, the fluorescent substrates resorufin benzyl ether, nile red, 7-benzyloxy-4-trifluoromethylcoumarin, dibenzylfluorescein, 7-benzyloxymethyloxy-3-cyanocoumarin, 7-benzyloxyquinoline, and dibenzyloxymethylfluorescein were examined and their metabolite formation by CYP3A7 was quantified using fitted fluorescent spectra. The maximum rates of reactions (Vmax) were determined for each substrate, along with the corresponding Michaelis-Menten constant (Km). Other characteristics, such as the Z-score and signal-to-noise ratio, were assessed to further demonstrate the utility of this methodology to screen for CYP3A7 activity in a high-throughput fashion. These findings will help determine which substrate is most useful for studies in heterogenous systems (i.e. human liver microsomes) and drug screening." @default.
- W3166335487 created "2021-06-22" @default.
- W3166335487 creator A5010372937 @default.
- W3166335487 creator A5021569962 @default.
- W3166335487 creator A5068700897 @default.
- W3166335487 date "2021-05-01" @default.
- W3166335487 modified "2023-09-27" @default.
- W3166335487 title "Development of a High‐throughput Fluorescent‐Based Assay to Assess Cytochrome P450 CYP3A7 Activity in Neonatal Human Liver Microsomes" @default.
- W3166335487 doi "https://doi.org/10.1096/fasebj.2021.35.s1.02177" @default.
- W3166335487 hasPublicationYear "2021" @default.
- W3166335487 type Work @default.
- W3166335487 sameAs 3166335487 @default.
- W3166335487 citedByCount "0" @default.
- W3166335487 crossrefType "journal-article" @default.
- W3166335487 hasAuthorship W3166335487A5010372937 @default.
- W3166335487 hasAuthorship W3166335487A5021569962 @default.
- W3166335487 hasAuthorship W3166335487A5068700897 @default.
- W3166335487 hasConcept C109650736 @default.
- W3166335487 hasConcept C115448650 @default.
- W3166335487 hasConcept C11824378 @default.
- W3166335487 hasConcept C181199279 @default.
- W3166335487 hasConcept C185592680 @default.
- W3166335487 hasConcept C18903297 @default.
- W3166335487 hasConcept C2777289219 @default.
- W3166335487 hasConcept C2777477808 @default.
- W3166335487 hasConcept C2780035454 @default.
- W3166335487 hasConcept C2908647359 @default.
- W3166335487 hasConcept C51323132 @default.
- W3166335487 hasConcept C526171541 @default.
- W3166335487 hasConcept C55493867 @default.
- W3166335487 hasConcept C71924100 @default.
- W3166335487 hasConcept C74187038 @default.
- W3166335487 hasConcept C86803240 @default.
- W3166335487 hasConcept C87644729 @default.
- W3166335487 hasConcept C89311334 @default.
- W3166335487 hasConcept C98274493 @default.
- W3166335487 hasConcept C99454951 @default.
- W3166335487 hasConceptScore W3166335487C109650736 @default.
- W3166335487 hasConceptScore W3166335487C115448650 @default.
- W3166335487 hasConceptScore W3166335487C11824378 @default.
- W3166335487 hasConceptScore W3166335487C181199279 @default.
- W3166335487 hasConceptScore W3166335487C185592680 @default.
- W3166335487 hasConceptScore W3166335487C18903297 @default.
- W3166335487 hasConceptScore W3166335487C2777289219 @default.
- W3166335487 hasConceptScore W3166335487C2777477808 @default.
- W3166335487 hasConceptScore W3166335487C2780035454 @default.
- W3166335487 hasConceptScore W3166335487C2908647359 @default.
- W3166335487 hasConceptScore W3166335487C51323132 @default.
- W3166335487 hasConceptScore W3166335487C526171541 @default.
- W3166335487 hasConceptScore W3166335487C55493867 @default.
- W3166335487 hasConceptScore W3166335487C71924100 @default.
- W3166335487 hasConceptScore W3166335487C74187038 @default.
- W3166335487 hasConceptScore W3166335487C86803240 @default.
- W3166335487 hasConceptScore W3166335487C87644729 @default.
- W3166335487 hasConceptScore W3166335487C89311334 @default.
- W3166335487 hasConceptScore W3166335487C98274493 @default.
- W3166335487 hasConceptScore W3166335487C99454951 @default.
- W3166335487 hasFunder F4320332161 @default.
- W3166335487 hasIssue "S1" @default.
- W3166335487 hasLocation W31663354871 @default.
- W3166335487 hasOpenAccess W3166335487 @default.
- W3166335487 hasPrimaryLocation W31663354871 @default.
- W3166335487 hasRelatedWork W1228620934 @default.
- W3166335487 hasRelatedWork W2021294637 @default.
- W3166335487 hasRelatedWork W2112843562 @default.
- W3166335487 hasRelatedWork W2156947160 @default.
- W3166335487 hasRelatedWork W2158345238 @default.
- W3166335487 hasRelatedWork W2179536258 @default.
- W3166335487 hasRelatedWork W2331785015 @default.
- W3166335487 hasRelatedWork W2952038621 @default.
- W3166335487 hasRelatedWork W2973640134 @default.
- W3166335487 hasRelatedWork W3048379644 @default.
- W3166335487 hasVolume "35" @default.
- W3166335487 isParatext "false" @default.
- W3166335487 isRetracted "false" @default.
- W3166335487 magId "3166335487" @default.
- W3166335487 workType "article" @default.