| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377338 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
The LPA2 protein is overexpressed in many tumor cells. We report the optimization of a series of LPA2 antagonists using calcium mobilization assay (aequorin assay) that led to the discovery of the first reported inhibitors selective for LPA2. Key compounds were evaluated in vitro for inhibition of LPA2 mediated Erk activation and proliferation of HCT-116 cells. These compounds could be used to evaluate the benefits of LPA2 inhibition both in vitro and in vivo.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Hilary P. Beck, Todd Kohn, Steven Rubenstein, Christine Hedberg, Ralf Schwandner, Kerstin Hasslinger, Kang Dai, Cong Li, Lingming Liang, Holger Wesche, Brendon Frank, Songhzu An, Dineli Wickramasinghe, Juan Jaen, Julio Medina, Randall Hungate, Wang Shen,