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| Reference : Paf-Receptor. 1. 'Cache-Oreilles' Effect of Selected High-Potency Platelet-Activating Fa... |
| Scientific journals : Article | |||
| Human health sciences : Pharmacy, pharmacology & toxicology Physical, chemical, mathematical & earth Sciences : Chemistry | |||
| http://hdl.handle.net/2268/30178 | |||
| Paf-Receptor. 1. 'Cache-Oreilles' Effect of Selected High-Potency Platelet-Activating Factor (Paf) Antagonists | |
| English | |
Dive, Georges  [Université de Liège - ULg > > Centre d'ingénierie des protéines >] | |
| Godfroid, Jean-Jacques [> > > >] | |
| Lamotte-Brasseur, Josette [> > > >] | |
| Batt, Jean-Pierre [> > > >] | |
| Heymans, Françoise [> > > >] | |
| Dupont, Léon [> > Cristallographie >] | |
| Braquet, Pierre [> > > >] | |
| 1989 | |
| Journal of Lipid Mediators | |
| 1 | |
| 4, Jul-Aug | |
| 201-15 | |
| International | |
| 0921-8319 | |
| [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. | |
| Researchers ; Professionals | |
| http://hdl.handle.net/2268/30178 |
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