Molecular basis for lysophosphatidic acid receptor antagonist selectivity

Vineet M. Sardar, Debra L. Bautista, David J. Fischer, Kazuaki Yokoyama, Nora Nusser, Tamas Virag, De An Wang, Daniel L. Baker, Gabor Tigyi, Abby L. Parrill

Research output: Contribution to journalReview article

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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 LPA 1 /EDG2 receptor (a benzyl-4-oxybenzyl N-acyl ethanolamide phosphate, NAEPA, derivative) and the other selective for the LPA 3 /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.

Original languageEnglish (US)
Pages (from-to)309-317
Number of pages9
JournalBiochimica et Biophysica Acta - Molecular and Cell Biology of Lipids
Volume1582
Issue number1-3
DOIs
StatePublished - May 23 2002

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Lysophosphatidic Acid Receptors
Structure-Activity Relationship
Phosphates
lysophosphatidic acid
diacylglycerol pyrophosphate

All Science Journal Classification (ASJC) codes

  • Molecular Biology
  • Cell Biology

Cite this

Sardar, V. M., Bautista, D. L., Fischer, D. J., Yokoyama, K., Nusser, N., Virag, T., ... Parrill, A. L. (2002). Molecular basis for lysophosphatidic acid receptor antagonist selectivity. Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids, 1582(1-3), 309-317. https://doi.org/10.1016/S1388-1981(02)00185-3

Molecular basis for lysophosphatidic acid receptor antagonist selectivity. / Sardar, Vineet M.; Bautista, Debra L.; Fischer, David J.; Yokoyama, Kazuaki; Nusser, Nora; Virag, Tamas; Wang, De An; Baker, Daniel L.; Tigyi, Gabor; Parrill, Abby L.

In: Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids, Vol. 1582, No. 1-3, 23.05.2002, p. 309-317.

Research output: Contribution to journalReview article

Sardar, VM, Bautista, DL, Fischer, DJ, Yokoyama, K, Nusser, N, Virag, T, Wang, DA, Baker, DL, Tigyi, G & Parrill, AL 2002, 'Molecular basis for lysophosphatidic acid receptor antagonist selectivity', Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids, vol. 1582, no. 1-3, pp. 309-317. https://doi.org/10.1016/S1388-1981(02)00185-3
Sardar, Vineet M. ; Bautista, Debra L. ; Fischer, David J. ; Yokoyama, Kazuaki ; Nusser, Nora ; Virag, Tamas ; Wang, De An ; Baker, Daniel L. ; Tigyi, Gabor ; Parrill, Abby L. / Molecular basis for lysophosphatidic acid receptor antagonist selectivity. In: Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids. 2002 ; Vol. 1582, No. 1-3. pp. 309-317.
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