Molecular basis for lysophosphatidic acid receptor antagonist selectivity
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. © 2002 Elsevier Science B.V. All rights reserved.
Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids
Sardar, V., Bautista, D., Fischer, D., Yokoyama, K., Nusser, N., Virag, T., Wang, D., & Baker, D. (2002). Molecular basis for lysophosphatidic acid receptor antagonist selectivity. Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids, 1582 (2022-01-03), 309-317. https://doi.org/10.1016/S1388-1981(02)00185-3