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Bioorg Med Chem Lett. 2008 Feb 1;18(3):1037-41. doi: 10.1016/j.bmcl.2007.12.024. Epub 2008 Jan 4.

Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents.

Author information

1
Chemistry Research & Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. hbeck@amgen.com

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.

PMID:
18178086
DOI:
10.1016/j.bmcl.2007.12.024
[Indexed for MEDLINE]

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