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

The LPA sub(2) protein is overexpressed in many tumor cells. We report the optimization of a series of LPA sub(2) antagonists using calcium mobilization assay (aequorin assay) that led to the discovery of the first reported inhibitors selective for LPA sub(2). Key compounds were evaluated in vitro f...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry 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 01.02.2008
Online AccessGet full text

Cover

More Information
Summary:The LPA sub(2) protein is overexpressed in many tumor cells. We report the optimization of a series of LPA sub(2) antagonists using calcium mobilization assay (aequorin assay) that led to the discovery of the first reported inhibitors selective for LPA sub(2). Key compounds were evaluated in vitro for inhibition of LPA sub(2) mediated Erk activation and proliferation of HCT-116 cells. These compounds could be used to evaluate the benefits of LPA sub(2) inhibition both in vitro and in vivo.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
content type line 23
ObjectType-Feature-2
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmcl.2007.12.024