Discovery of potent LPA 2 (EDG4) antagonists as potential anticancer agents

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 o...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 18; no. 3; pp. 1037 - 1041
Main Authors Beck, Hilary P., Kohn, Todd, Rubenstein, Steven, Hedberg, Christine, Schwandner, Ralf, Hasslinger, Kerstin, Dai, Kang, Li, Cong, Liang, Lingming, Wesche, Holger, Frank, Brendon, An, Songhzu, Wickramasinghe, Dineli, Jaen, Juan, Medina, Julio, Hungate, Randall, Shen, Wang
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 2008
Subjects
Anticancer agents
EDG4
LPA
LPA2
LPA2
Anticancer agents
EDG4
LPA
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.12.024