| Literature DB >> 14667211 |
Lian Qian1, Yong Xu, Yutaka Hasegawa, Junken Aoki, Gordon B Mills, Glenn D Prestwich.
Abstract
The metabolically stabilized LPA analogue, 1-oleoyl-2-O-methyl-rac-glycerophosphothioate (OMPT), is a potent agonist for the LPA(3) G-protein-coupled receptor. A new enantiospecific synthesis of both (2R)-OMPT and (2S)-OMPT is described. Calcium release assays in both LPA(3)-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.Entities:
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Year: 2003 PMID： 14667211 DOI： 10.1021/jm034207p
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446