Enantioselective Responses to a Phosphorothioate Analogue of Lysophosphatidic Acid with LPA3 Receptor-Selective Agonist Activity

Lian Qian, Yong Xu, Yutaka Hasegawa, Junken Aoki, Gordon B. Mills, Glenn D. Prestwich

    Research output: Contribution to journalArticle

    52 Scopus citations

    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 languageEnglish (US)
    Pages (from-to)5575-5578
    Number of pages4
    JournalJournal of Medicinal Chemistry
    Volume46
    Issue number26
    DOIs
    StatePublished - Dec 18 2003

    ASJC Scopus subject areas

    • Molecular Medicine
    • Drug Discovery

    Fingerprint Dive into the research topics of 'Enantioselective Responses to a Phosphorothioate Analogue of Lysophosphatidic Acid with LPA<sub>3</sub> Receptor-Selective Agonist Activity'. Together they form a unique fingerprint.

  • Cite this