Phosphorothioate analogs of sn-2 radyl lysophosphatidic acid (LPA): metabolically stabilized LPA receptor agonists

G Jiang, A Inoue, J Aoki, GD Prestwich

Index: Jiang, Guowei; Inoue, Asuka; Aoki, Junken; Prestwich, Glenn D. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1865 - 1869

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Citation Number: 13

Abstract

We describe an efficient synthesis of metabolically stabilized sn-2 radyl phosphorothioate analogs of lysophosphatidic acid (LPA), and the determination of the agonist activity of each analog for the six LPA receptors (LPA1–6) using a recently developed TGFα shedding assay. In general, the sn-2 radyl OMPT analogs showed similar agonist activities to the previous 1-oleoyl-2-O-methyl-glycerophosphothioate (sn-1 OMPT) analogs for LPA1–6 ...