Author/Authors :
Hilary P. Beck، نويسنده , , Todd Kohn، نويسنده , , Steven Rubenstein، نويسنده , , Christine Hedberg، نويسنده , , Ralf Schwandner، نويسنده , , Kerstin Hasslinger، نويسنده , , Kang Dai، نويسنده , , Cong Li، نويسنده , , Lingming Liang، نويسنده , , Holger Wesche، نويسنده , , Brendon Frank، نويسنده , , Songhzu An، نويسنده , , Dineli Wickramasinghe، نويسنده , , Juan Jaen، نويسنده , , Julio Medina، نويسنده , , Randall Hungate، نويسنده , , Wang Shen، نويسنده ,
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.
Keywords :
LPA2 , LPA , anticancer agents , EDG4
