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| Reference : Paf-Receptor. iii. Conformational and Electronic Properties of Paf-Like Agonists and Ant... |
| Scientific journals : Article | |||
| Physical, chemical, mathematical & earth Sciences : Chemistry | |||
| http://hdl.handle.net/2268/30179 | |||
| Paf-Receptor. iii. Conformational and Electronic Properties of Paf-Like Agonists and Antagonists | |
| English | |
| Lamotte-Brasseur, Josette [> > > >] | |
Dive, Georges  [Université de Liège - ULg > > Centre d'ingénierie des protéines >] | |
| Lamouri, Aazdine [> > > >] | |
| Heymans, Françoise [> > > >] | |
| Godfroid, Jean-Jacques [> > > >] | |
| 20-Aug-1991 | |
| Biochimica et Biophysica Acta | |
| 1085 | |
| 1 | |
| 91-105 | |
| International | |
| 0006-3002 | |
| [en] In order to compare electronic and conformational properties of PAF-agonists and PAF-antagonists, 14 analogues structurally related to PAF were studied. A common conformation of the glycerol backbone was present in all agonists and all constrained or flexible antagonists. The distinction between agonists and antagonists appears to be casted on position-2 where the folded conformation of the substituent for agonists should be the most probable. In position-3 the gauche conformation can be adopted by all the analysed compounds. The electrostatic potential well at -30 kcal/mol stretches to the carbonyl group in position-2 in the folded conformation of the agonists. On the contrary, in constrained antagonists, a second negative zone appears around the carbamate group. Given the modelling results, the triethylammonium PAF analogue considered in literature as a weak agonist, was resynthesized and proved to be more potent than previously reported. These experimental results confirm our hypothesis in terms of a common conformation of agonist and antagonist PAF-like molecules. | |
| Researchers ; Professionals | |
| http://hdl.handle.net/2268/30179 |
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