Matches in SemOpenAlex for { <https://semopenalex.org/work/W2112170341> ?p ?o ?g. }
Showing items 1 to 94 of
94
with 100 items per page.
- W2112170341 endingPage "94" @default.
- W2112170341 startingPage "3089" @default.
- W2112170341 abstract "The anticancer drug CPT-11 (7-ethyl-[4(1-piperidino)-1-piperidino]carbonyloxycamptothecin) is a water-soluble derivative of camptothecin. We report here the conversion of APC (7-ethyl-[4-N-(5-aminopentanoic acid)-1-piperidino] carbonyloxycamptothecin), an inactive metabolite of CPT-11, to SN-38 (7-ethyl-10-hydroxycamptothecin), the active metabolite of CPT-11, by a rabbit liver carboxylesterase. This reaction is not catalyzed by any known human enzyme. The formation of SN-38 from APC was characterized by an apparent Km of 37.9 +/- 7.1 microM and a Vmax of 16.9 +/- 0.9 pmol/units/min. SN-38 was confirmed as a reaction product by high-performance liquid chromatography and mass spectrometry. A 24-h incubation of 10 microM APC with 500 units/ml of rabbit carboxylesterase produced 4 microM SN-38. The product of this reaction inhibited the growth of U373 MG human glioblastoma cells in vitro. The IC50 for a 24-h exposure of U373 MG cells to APC in the presence of 50 units/ml of rabbit carboxylesterase was 0.27 +/- 0.08 microM, whereas APC alone demonstrated no inhibition of growth at concentrations up to 1 microM. The IC50 of U373 MG cells transfected with the cDNA encoding the rabbit carboxylesterase (U373pIRESrabbit) and exposed to APC for 24 h was 0.8 +/- 0.1 microM APC, whereas the growth of cells transfected with vector control (U373pIRES) was unaffected by up to 1 microM APC. Because APC is nontoxic to human cells, we are investigating the possibility of using APC/rabbit carboxylesterase in a prodrug/enzyme therapeutic approach." @default.
- W2112170341 created "2016-06-24" @default.
- W2112170341 creator A5032094946 @default.
- W2112170341 creator A5032991502 @default.
- W2112170341 creator A5040373927 @default.
- W2112170341 creator A5043293908 @default.
- W2112170341 creator A5066877678 @default.
- W2112170341 creator A5083486073 @default.
- W2112170341 date "1998-12-01" @default.
- W2112170341 modified "2023-09-23" @default.
- W2112170341 title "Conversion of the CPT-11 metabolite APC to SN-38 by rabbit liver carboxylesterase." @default.
- W2112170341 cites W106814647 @default.
- W2112170341 cites W1521764325 @default.
- W2112170341 cites W1523357361 @default.
- W2112170341 cites W1557866953 @default.
- W2112170341 cites W1697277777 @default.
- W2112170341 cites W1964677552 @default.
- W2112170341 cites W1994399615 @default.
- W2112170341 cites W1996671757 @default.
- W2112170341 cites W2013319406 @default.
- W2112170341 cites W2016722642 @default.
- W2112170341 cites W2019867999 @default.
- W2112170341 cites W2035051990 @default.
- W2112170341 cites W2070781613 @default.
- W2112170341 cites W2111198194 @default.
- W2112170341 cites W2144473674 @default.
- W2112170341 cites W2159634500 @default.
- W2112170341 cites W2162062930 @default.
- W2112170341 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9865925" @default.
- W2112170341 hasPublicationYear "1998" @default.
- W2112170341 type Work @default.
- W2112170341 sameAs 2112170341 @default.
- W2112170341 citedByCount "15" @default.
- W2112170341 countsByYear W21121703412014 @default.
- W2112170341 crossrefType "journal-article" @default.
- W2112170341 hasAuthorship W2112170341A5032094946 @default.
- W2112170341 hasAuthorship W2112170341A5032991502 @default.
- W2112170341 hasAuthorship W2112170341A5040373927 @default.
- W2112170341 hasAuthorship W2112170341A5043293908 @default.
- W2112170341 hasAuthorship W2112170341A5066877678 @default.
- W2112170341 hasAuthorship W2112170341A5083486073 @default.
- W2112170341 hasConcept C121608353 @default.
- W2112170341 hasConcept C149151106 @default.
- W2112170341 hasConcept C153911025 @default.
- W2112170341 hasConcept C181199279 @default.
- W2112170341 hasConcept C185592680 @default.
- W2112170341 hasConcept C2776980637 @default.
- W2112170341 hasConcept C2777477808 @default.
- W2112170341 hasConcept C2778325069 @default.
- W2112170341 hasConcept C2779682216 @default.
- W2112170341 hasConcept C2780259306 @default.
- W2112170341 hasConcept C2780508388 @default.
- W2112170341 hasConcept C526805850 @default.
- W2112170341 hasConcept C54355233 @default.
- W2112170341 hasConcept C55493867 @default.
- W2112170341 hasConcept C81885089 @default.
- W2112170341 hasConcept C86803240 @default.
- W2112170341 hasConceptScore W2112170341C121608353 @default.
- W2112170341 hasConceptScore W2112170341C149151106 @default.
- W2112170341 hasConceptScore W2112170341C153911025 @default.
- W2112170341 hasConceptScore W2112170341C181199279 @default.
- W2112170341 hasConceptScore W2112170341C185592680 @default.
- W2112170341 hasConceptScore W2112170341C2776980637 @default.
- W2112170341 hasConceptScore W2112170341C2777477808 @default.
- W2112170341 hasConceptScore W2112170341C2778325069 @default.
- W2112170341 hasConceptScore W2112170341C2779682216 @default.
- W2112170341 hasConceptScore W2112170341C2780259306 @default.
- W2112170341 hasConceptScore W2112170341C2780508388 @default.
- W2112170341 hasConceptScore W2112170341C526805850 @default.
- W2112170341 hasConceptScore W2112170341C54355233 @default.
- W2112170341 hasConceptScore W2112170341C55493867 @default.
- W2112170341 hasConceptScore W2112170341C81885089 @default.
- W2112170341 hasConceptScore W2112170341C86803240 @default.
- W2112170341 hasIssue "12" @default.
- W2112170341 hasLocation W21121703411 @default.
- W2112170341 hasOpenAccess W2112170341 @default.
- W2112170341 hasPrimaryLocation W21121703411 @default.
- W2112170341 hasRelatedWork W1485886034 @default.
- W2112170341 hasRelatedWork W2013319406 @default.
- W2112170341 hasRelatedWork W2028511849 @default.
- W2112170341 hasRelatedWork W2059224614 @default.
- W2112170341 hasRelatedWork W2076554129 @default.
- W2112170341 hasRelatedWork W2112170341 @default.
- W2112170341 hasRelatedWork W2321350829 @default.
- W2112170341 hasRelatedWork W2328209945 @default.
- W2112170341 hasRelatedWork W4210875954 @default.
- W2112170341 hasRelatedWork W2053856090 @default.
- W2112170341 hasVolume "4" @default.
- W2112170341 isParatext "false" @default.
- W2112170341 isRetracted "false" @default.
- W2112170341 magId "2112170341" @default.
- W2112170341 workType "article" @default.