Document Detail

Lysophosphatidic acid (LPA) receptors of the EDG family are differentially activated by LPA species. Structure-activity relationship of cloned LPA receptors.
MedLine Citation:
PMID:  10922489     Owner:  NLM     Status:  MEDLINE    
We examined the structure-activity relationship of cloned lysophosphatidic acid (LPA) receptors (endothelial cell differentiation gene (EDG) 2, EDG4, and EDG7) by measuring [Ca(2+)](i) in Sf9 insect cells expressing each receptor using LPA with various acyl chains bound at either the sn-1 or the sn-2 position of the glycerol backbone. For EDG7 the highest reactivity was observed with LPA with Delta9-unsaturated fatty acid (oleic (18:1), linoleic (18:2), and linolenic (18:3)) at sn-2 followed by 2-palmitoleoyl (16:1) and 2-arachidonoyl (20:4) LPA. In contrast, EDG2 and EDG4 showed broad ligand specificities, although EDG2 and EDG4 discriminated between 14:0 (myristoyl) and 16:0 (palmitoyl), and 12:0 (lauroyl) and 14:0 LPAs, respectively. EDG7 recognizes the cis double bond at the Delta9 position of octadecanoyl residues, since 2-elaidoyl (18:1, trans) and 2-petroselinoyl (18:1, cis-Delta12) LPA were poor ligands for EDG7. In conclusion, the present study demonstrates that each LPA receptor can be activated differentially by the LPA species.
K Bandoh; J Aoki; A Taira; M Tsujimoto; H Arai; K Inoue
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  FEBS letters     Volume:  478     ISSN:  0014-5793     ISO Abbreviation:  FEBS Lett.     Publication Date:  2000 Jul 
Date Detail:
Created Date:  2000-08-29     Completed Date:  2000-08-29     Revised Date:  2005-11-17    
Medline Journal Info:
Nlm Unique ID:  0155157     Medline TA:  FEBS Lett     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  159-65     Citation Subset:  IM    
Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
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MeSH Terms
Amino Acid Sequence
Calcium / metabolism
Calcium Signaling / drug effects
Cell Line
Dose-Response Relationship, Drug
Lysophospholipids / chemistry,  pharmacology*
Molecular Sequence Data
Receptors, Cell Surface / chemistry,  genetics,  metabolism*
Receptors, G-Protein-Coupled*
Receptors, Lysophosphatidic Acid
Recombinant Fusion Proteins / chemistry,  genetics,  metabolism
Structure-Activity Relationship
Substrate Specificity
Reg. No./Substance:
0/Ligands; 0/Lysophospholipids; 0/Receptors, Cell Surface; 0/Receptors, G-Protein-Coupled; 0/Receptors, Lysophosphatidic Acid; 0/Recombinant Fusion Proteins; 7440-70-2/Calcium

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