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Discovery of potent and practical antiangiogenic agents inspired by cortistatin A

Journal of the American Chemical Society, ISSN: 0002-7863, Vol: 131, Issue: 25, Page: 9014-9019
2009
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Article Description

The discovery that cortistatins A and J show noteworthy antiangiogenic activity prompted an investigation of the possibility that simpler and much more easily made compounds based on a steroid core might have useful bioactivity. These studies have led to the development of several potent, watersoluble compounds that may be suitable for local application to treat ocular wet macular degeneration, an important cause of blindness, as well as for treatment of various other angiogenesis-dependent diseases. One of these substances was tested in a mouse retinal angiogenesis model and found to inhibit angiogenesis at a locally administered dose of 500 pmol. Comparison of cell migration data for this and two other synthetic compounds with published data on cortistatin A indicate that they inhibit vascular endothelial growth factorinduced cell migration of human umbilical vein endothelial cells more strongly than cortistatin A. © 2009 American Chemical Society.

Bibliographic Details

Czakó, Barbara; Kürti, László; Mammoto, Akiko; Ingber, Donald E; Corey, E J

American Chemical Society (ACS)

Chemical Engineering; Chemistry; Biochemistry, Genetics and Molecular Biology

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