Discovery of potent and practical antiangiogenic agents inspired by cortistatin A

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

Research output: Contribution to journalArticle

52 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)9014-9019
Number of pages6
JournalJournal of the American Chemical Society
Volume131
Issue number25
DOIs
StatePublished - Jul 1 2009

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)
  • Biochemistry
  • Colloid and Surface Chemistry

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