Reference : Paf-Receptor. iii. Conformational and Electronic Properties of Paf-Like Agonists and ...
Scientific journals : Article
Physical, chemical, mathematical & earth Sciences : Chemistry
Paf-Receptor. iii. Conformational and Electronic Properties of Paf-Like Agonists and Antagonists
Lamotte-Brasseur, Josette [> > > >]
Dive, Georges [Université de Liège - ULiège > > Centre d'ingénierie des protéines >]
Lamouri, Aazdine [> > > >]
Heymans, Françoise [> > > >]
Godfroid, Jean-Jacques [> > > >]
Biochimica et Biophysica Acta
Yes (verified by ORBi)
[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.
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