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The VEGFR 2 inhibitor SU1498 stimulates ERK kinase accumulation and inhibition.

Women's Health Weekly

| April 01, 2004 | COPYRIGHT 2004 NewsRX. This material is published under license from the publisher through the Gale Group, Farmington Hills, Michigan.  All inquiries regarding rights should be directed to the Gale Group. (Hide copyright information)Copyright

2004 APR 1 - (NewsRx.com & NewsRx.net) -- The VEGFR 2 inhibitor SU1498 stimulates ERK kinase accumulation and inhibition.

"SU1498, an inhibitor of vascular endothelial growth factor receptor 2, has been used successfully to study the physiological manifestations of receptor functions. Here we report that in addition to its anti-receptor activity, SU1498 stimulates accumulation of phosphorylated extracellular regulated kinases (ERKs) in human umbilical vein endothelial cells and in human aortic endothelial cells in a manner that is dependent on the functioning of the upstream components of the MAPK pathway, B-Raf, and MEK kinases," according to scientists in the United States.

"The enhanced accumulation of phospho-ERKs is observed only in cells that have been stimulated with sphingosine 1-phosphate or protein growth factors; SU1498 by itself is ineffective," noted G. Boguslawski and colleagues, Indiana University, School of Medicine.

"We show that the inhibitor acts by blocking the kinase activity of phospho-ERK both in a direct assay and in immunoprecipitates from cells treated ...

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