1985
DOI: 10.1016/0006-291x(85)91156-8
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Inhibition of transmembrane movement and metabolism of platelet activating factor (PAF-acether) by a specific antagonist, BN 52021

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Cited by 39 publications
(14 citation statements)
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“…Pharmacological suppression of ␣ 1 by BN 52021 or FR 49175 accelerates the kinetics of PAF deacetylation to lyso-PAF and protects cells from PAF-mediated apoptosis. Although it would at first appear counterintuitive that a reduction in PAF-AH subunit expression enhances PAF hydrolysis, these data are consistent with previous reports that BN 52021 inhibits PAF degradation under nonapoptotic culture conditions (48,50). PAF-AH I ␣ 2 /␣ 2 is known to hydrolyze PAF more efficiently than ␣ 1 /␣ 1 homodimers, and it is likely that reducing PAF-AH ␣ 1 coincident with PAF-AH ␣ 2 induction would promote more rapid formation of ␣ 2 /␣ 2 homodimers, enhance PAF hydrolysis, and increase cell survival.…”
Section: Cytosolic Paf-ahs Can Be Targeted Pharmacologically To Promosupporting
confidence: 91%
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“…Pharmacological suppression of ␣ 1 by BN 52021 or FR 49175 accelerates the kinetics of PAF deacetylation to lyso-PAF and protects cells from PAF-mediated apoptosis. Although it would at first appear counterintuitive that a reduction in PAF-AH subunit expression enhances PAF hydrolysis, these data are consistent with previous reports that BN 52021 inhibits PAF degradation under nonapoptotic culture conditions (48,50). PAF-AH I ␣ 2 /␣ 2 is known to hydrolyze PAF more efficiently than ␣ 1 /␣ 1 homodimers, and it is likely that reducing PAF-AH ␣ 1 coincident with PAF-AH ␣ 2 induction would promote more rapid formation of ␣ 2 /␣ 2 homodimers, enhance PAF hydrolysis, and increase cell survival.…”
Section: Cytosolic Paf-ahs Can Be Targeted Pharmacologically To Promosupporting
confidence: 91%
“…In addition to endocytosis as a PAF⅐PAFR complex, active trafficking of PAF across the plasma membrane is accomplished by a PAF-specific transglutaminase and by interaction with low affinity binding sites yet to be identified at the molecular level (14,48). Passive PAF internalization is regulated by transbilayer movement (flipping) across the plasma membrane occurring as a result of physicochemical changes in membrane properties accompanying cellular activation (15).…”
Section: Cytosolic Paf-ahs Can Be Targeted Pharmacologically To Promomentioning
confidence: 99%
“…These binding data are further corroborated by the results on the inhibition of PAF-induced aggregation of washed human (Braquet, 1984 These data are correlated with the inhibition by BN 52021 of both reacylation of lyso-PAF into 1-0-alkyl- (Lachachi et al, 1985) and phosphatidic acid synthesis (Simon et al, 1987) in intact rabbit platelets, without inhibition of acetyltransferase. Furthermore, a significant decrease in PAF-induced [Ca2+]i, as measured by the fluorescent probe Quin-2 has been recorded in rabbit platelets treated with BN 52021 (Baroggi et al, 1985;Simon et al, 1987).…”
Section: Effects On Platelet Aggregation and Thrombosissupporting
confidence: 54%
“…1), suggesting the functional significance of the receptor-dependent degradation mechanism. A PAF antagonist, BN 52021, was previously reported to decrease PAF degradation activity of rabbit platelets (40,41). By tracing [ 3 H]PAF, we showed that PAF was internalized very rapidly with PAF receptor (Fig.…”
Section: Discussionmentioning
confidence: 69%