Pefabloc, 4-[2-aminoethyl]benzenesulfonyl fluoride, is a new, potent nontoxic and irreversible inhibitor of PAF-degrading acetylhydrolase

dc.contributor.authorDentan, C.en
dc.contributor.authorTselepis, A. D.en
dc.contributor.authorChapman, M. J.en
dc.contributor.authorNinio, E.en
dc.date.accessioned2015-11-24T16:44:07Z
dc.date.available2015-11-24T16:44:07Z
dc.identifier.issn0005-2760-
dc.identifier.urihttps://olympias.lib.uoi.gr/jspui/handle/123456789/8773
dc.rightsDefault Licence-
dc.subjectpafen
dc.subjectacetylhydrolaseen
dc.subjectpefablocen
dc.subjectinflammatory mediatoren
dc.subjectlipoproteinen
dc.subjectplatelet-activating-factoren
dc.subjecthuman-plasmaen
dc.subjecthuman-serumen
dc.subjectmacrophagesen
dc.subjectacetheren
dc.subjectlipoproteinsen
dc.subjectdegradationen
dc.titlePefabloc, 4-[2-aminoethyl]benzenesulfonyl fluoride, is a new, potent nontoxic and irreversible inhibitor of PAF-degrading acetylhydrolaseen
heal.abstractWe report here that 4-[2-aminoethyl]benzenesulfonyl fluoride (Pefabloc SC, Pefabloc), a new irreversible serine proteinase inhibitor, efficiently inhibits both human and rat platelet activating factor (PAF)-degrading acetylhydrolase (acetylhydrolase). Indeed, low concentrations of Pefabloc (0.1 mM) rapidly and totally inactivate both human plasma-, VLDL-, IDL-, LDL- and HDL-associated acetylhydrolase, and in addition, acetylhydrolase synthesized and released by human adherent monocytes in culture, as well as rat brain cytosolic acetylhydrolase. By contrast, Pefabloc only minimally inhibited the phospholipase A(2) (PLA(2)) activity from Naja naja and from porcine pancreas. In addition, Pefabloc is relatively nontoxic, stable and convenient to use. Henceforth, Pefabloc may replace both DFP and PMSF and therefore constitutes a useful and valuable tool in future studies of acetylhydrolase.en
heal.accesscampus-
heal.fullTextAvailabilityTRUE-
heal.identifier.secondary<Go to ISI>://A1996TX50200010-
heal.identifier.secondaryhttp://ac.els-cdn.com/000527609500226X/1-s2.0-000527609500226X-main.pdf?_tid=a32f72c63742466c77d9338f80cc0519&acdnat=1333111086_d9dab053d1010dc71ca18d6c0a84cd6d-
heal.journalNameBiochimica Et Biophysica Acta-Lipids and Lipid Metabolismen
heal.journalTypepeer reviewed-
heal.languageen-
heal.publicationDate1996-
heal.recordProviderΠανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείαςel
heal.typejournalArticle-
heal.type.elΆρθρο Περιοδικούel
heal.type.enJournal articleen

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