2. Academic Validation
  3. Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents

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

  • Bioorg Med Chem Lett. 2008 Feb 1;18(3):1037-41. doi: 10.1016/j.bmcl.2007.12.024.
Hilary P Beck 1,  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
Affiliations

Affiliation

  • 1 Chemistry Research & Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. [email protected]
PMID: 18178086 DOI: 10.1016/j.bmcl.2007.12.024
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.

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