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Paf-Receptor. iii. Conformational and Electronic Properties of Paf-Like Agonists and Antagonists
Lamotte-Brasseur, Josette; Dive, Georges; Lamouri, Aazdine et al.
1991In Biochimica et Biophysica Acta, 1085 (1), p. 91-105
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Abstract :
[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.
Disciplines :
Chemistry
Author, co-author :
Lamotte-Brasseur, Josette 
Dive, Georges ;  Université de Liège - ULiège > Centre d'ingénierie des protéines
Lamouri, Aazdine
Heymans, Françoise
Godfroid, Jean-Jacques
Language :
English
Title :
Paf-Receptor. iii. Conformational and Electronic Properties of Paf-Like Agonists and Antagonists
Publication date :
20 August 1991
Journal title :
Biochimica et Biophysica Acta
ISSN :
0006-3002
eISSN :
1878-2434
Publisher :
Elsevier, Amsterdam, Netherlands
Volume :
1085
Issue :
1
Pages :
91-105
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 30 November 2009

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