Lysophosphatidic acid (LPA) receptors of the EDG family are differentially activated by LPA species. Structure-activity relationship of cloned LPA receptors. | |
MedLine Citation:
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PMID: 10922489 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
Authors:
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K Bandoh; J Aoki; A Taira; M Tsujimoto; H Arai; K Inoue |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: FEBS letters Volume: 478 ISSN: 0014-5793 ISO Abbreviation: FEBS Lett. Publication Date: 2000 Jul |
Date Detail:
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Created Date: 2000-08-29 Completed Date: 2000-08-29 Revised Date: 2005-11-17 |
Medline Journal Info:
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Nlm Unique ID: 0155157 Medline TA: FEBS Lett Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 159-65 Citation Subset: IM |
Affiliation:
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Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan. |
Data Bank Information | |
Bank Name/Acc. No.:
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GENBANK/AF233092 |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
MeSH Terms | |
Descriptor/Qualifier:
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Amino Acid Sequence Animals Calcium / metabolism Calcium Signaling / drug effects Cell Line Dose-Response Relationship, Drug Humans Ligands 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 Spodoptera Structure-Activity Relationship Substrate Specificity Transfection |
Chemical | |
Reg. No./Substance:
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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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