Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp

J Nat Prod. 2013 Apr 26;76(4):715-9. doi: 10.1021/np300535c. Epub 2013 Feb 15.

Abstract

A new inhibitor of VEGF receptor tyrosine kinases, vegfrecine (1), was isolated from the culture broth of Streptomyces sp. MK931-CF8. The molecular structure of 1 was determined by NMR and MS analysis combined with synthesis. Compound 1 showed potent inhibitory activity against vascular endothelial growth factor receptor (VEGFR) tyrosine kinases in in vitro enzyme assays, but platelet-derived growth factor receptors (PDGFRs), fibroblast growth factor receptor (FGFR), and epidermal growth factor receptor (EGFR) responded only weakly. Compound 1 is a promising new selective VEGFR inhibitor for investigating new treatments of cancer and inflammatory diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzoquinones / chemistry
  • Benzoquinones / pharmacology*
  • Humans
  • Immunoblotting
  • Japan
  • Mice
  • Molecular Structure
  • NIH 3T3 Cells
  • Nuclear Magnetic Resonance, Biomolecular
  • Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Receptor Protein-Tyrosine Kinases / metabolism
  • Receptors, Vascular Endothelial Growth Factor / antagonists & inhibitors*
  • Receptors, Vascular Endothelial Growth Factor / metabolism
  • Streptomyces / chemistry*

Substances

  • Benzoquinones
  • vegfrecine
  • Receptor Protein-Tyrosine Kinases
  • Receptors, Vascular Endothelial Growth Factor