Reference : Paf-Receptor. 1. 'Cache-Oreilles' Effect of Selected High-Potency Platelet-Activating...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
Physical, chemical, mathematical & earth Sciences : Chemistry
Paf-Receptor. 1. 'Cache-Oreilles' Effect of Selected High-Potency Platelet-Activating Factor (Paf) Antagonists
Dive, Georges [Université de Liège - ULiège > > Centre d'ingénierie des protéines >]
Godfroid, Jean-Jacques [> > > >]
Lamotte-Brasseur, Josette [> > > >]
Batt, Jean-Pierre [> > > >]
Heymans, Françoise [> > > >]
Dupont, Léon mailto [> > Cristallographie >]
Braquet, Pierre [> > > >]
Journal of Lipid Mediators
4, Jul-Aug
Yes (verified by ORBi)
[en] Three-dimensional electrostatic maps were calculated for six potent antagonists of platelet-activating factor (PAF), the antagonists being selected for their apparent structural heterogeneity. The molecules examined were the compact Ginkgolides BN 52020, BN 52021 and BN 52022 (1, 2 and 3), the semi-rigid kadsurenone (4), a flexible synthetic dinor type C furanoid lignan L-652,731 (5a) and the triazolothienobenzodiazepine WEB 2086 (7). Calculation of the electrostatic potential generated around all the above molecules showed the existence of two wells of negative potential or 'cache-oreilles' (ear-muffs), i.e., the isocontours drawn at -10 kcal/mol, located at 180 degrees from each other and separated by a maximum distance of 22-27 A. Except for the synthetic dinor type C furanoid lignan (5a), the molecules also presented a moderate hydrophobic fragment, which constitutes a third point of interaction with the high-affinity binding site in rabbit and human platelets. The findings of the present study allow speculation that this high-affinity acceptor site may be a 'polarized cylinder' with a diameter of 10-12 A.
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