2. Academic Validation
  3. Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp

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.
Chisato Nosaka 1,  Hayamitsu Adachi,  Ryuichi Sawa,  Koichi Nakae,  Sonoko Atsumi,  Naoko Kinoshita,  Yumiko Kubota,  Masayuki Igarashi,  Yoshihisa Sei,  Kentaro Yamaguchi,  Masabumi Shibuya,  Yoshio Nishimura,  Yuzuru Akamatsu
Affiliations

Affiliation

  • 1 Institute of Microbial Chemistry (BIKAKEN), Tokyo, 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
PMID: 23414235 DOI: 10.1021/np300535c
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.

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