Abstract
The metabolically stabilized LPA analogue, 1-oleoyl-2-O-methyl-rac-glycerophosphothioate (OMPT), is a potent agonist for the LPA3 G-protein-coupled receptor. A new enantiospecific synthesis of both (2R)-OMPT and (2S)-OMPT is described. Calcium release assays in both LPA3-transfected insect Sf9 and rat hepatoma Rh7777 cells showed that (2S)-OMPT was 5- to 20-fold more active than (2R)-OMPT. Similar results were found for calcium release, MAPK and Akt activation, and IL-6 release in human OVCAR3 ovarian cancer cells.
Original language | English (US) |
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Pages (from-to) | 5575-5578 |
Number of pages | 4 |
Journal | Journal of Medicinal Chemistry |
Volume | 46 |
Issue number | 26 |
DOIs | |
State | Published - Dec 18 2003 |
Externally published | Yes |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery