title: Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp.
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.
authors: Institute of Microbial Chemistry (BIKAKEN), Tokyo, 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
authors: Chisato
authors: C
authors: Nosaka
authors: Hayamitsu
authors: H
authors: Adachi
authors: Ryuichi
authors: R
authors: Sawa
authors: Koichi
authors: K
authors: Nakae
authors: Sonoko
authors: S
authors: Atsumi
authors: Naoko
authors: N
authors: Kinoshita
authors: Yumiko
authors: Y
authors: Kubota
authors: Masayuki
authors: M
authors: Igarashi
authors: Yoshihisa
authors: Y
authors: Sei
authors: Kentaro
authors: K
authors: Yamaguchi
authors: Masabumi
authors: M
authors: Shibuya
authors: Yoshio
authors: Y
authors: Nishimura
authors: Yuzuru
authors: Y
authors: Akamatsu
mesh_terms: D000818:Animals; D016227:Benzoquinones / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015151:Immunoblotting; D007564:Japan; D051379:Mice; D015394:Molecular Structure; D041681:NIH 3T3 Cells; D019906:Nuclear Magnetic Resonance, Biomolecular; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D040262:Receptors, Vascular Endothelial Growth Factor / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013302:Streptomyces / Q000737:chemistry*
chemical_list: D016227:Benzoquinones; C582687:vegfrecine; D020794:Receptor Protein-Tyrosine Kinases; D040262:Receptors, Vascular Endothelial Growth Factor