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  • Title: Molecular basis for lysophosphatidic acid receptor antagonist selectivity.
    Author: Sardar VM, Bautista DL, Fischer DJ, Yokoyama K, Nusser N, Virag T, Wang DA, Baker DL, Tigyi G, Parrill AL.
    Journal: Biochim Biophys Acta; 2002 May 23; 1582(1-3):309-17. PubMed ID: 12069842.
    Abstract:
    Recent characterization of lysophosphatidic acid (LPA) receptors has made possible studies elucidating the structure-activity relationships (SAR) for agonist activity at individual receptors. Additionally, the availability of these receptors has allowed the identification of antagonists of LPA-induced effects. Two receptor-subtype selective LPA receptor antagonists, one selective for the LPA1/EDG2 receptor (a benzyl-4-oxybenzyl N-acyl ethanolamide phosphate, NAEPA, derivative) and the other selective for the LPA3/EDG7 receptor (diacylglycerol pyrophosphate, DGPP, 8:0), have recently been reported. The receptor SAR for both agonists and antagonists are reviewed, and the molecular basis for the difference between agonism and antagonism as well as for receptor-subtype antagonist selectivity identified by molecular modeling is described. The implications of the newly available receptor-subtype selective antagonists are also discussed.
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