Document Report Card
Basic Information
ID: ALA1143154
Journal: Bioorg Med Chem Lett
Title: Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents.
Authors: Beck HP, Kohn T, Rubenstein S, Hedberg C, Schwandner R, Hasslinger K, Dai K, Li C, Liang L, Wesche H, Frank B, An S, Wickramasinghe D, Jaen J, Medina J, Hungate R, Shen W.
Abstract: The LPA(2) protein is overexpressed in many tumor cells. We report the optimization of a series of LPA(2) antagonists using calcium mobilization assay (aequorin assay) that led to the discovery of the first reported inhibitors selective for LPA(2). Key compounds were evaluated in vitro for inhibition of LPA(2) mediated Erk activation and proliferation of HCT-116 cells. These compounds could be used to evaluate the benefits of LPA(2) inhibition both in vitro and in vivo.
CiteXplore: 18178086