Inhibition of angiogenesis by erbstatin, an inhibitor of tyrosine kinase.
Here we describe the inhibitory effect of erbstatin, a specific tyrosine kinase inhibitor, on in vivo angiogenesis. Inhibition of angiogenesis was determined in a bioassay system involving chorioallantoic membranes of growing chick embryos. Erbstatin produced a dose-dependent inhibitory action on embryonic angiogenesis. This inhibition occurred at as small a dose as 10 ng/egg and the ID50 value was 80 ng/egg. To analyze this inhibition, in vitro experiments involving vascular endothelial cells were also performed. Erbstatin affected the proliferation of vascular endothelial cells, one of angiogenic components. This inhibition was dose-dependent, the IC50 value being 3.6 microM. These data indicate that erbstatin-sensitive tyrosine kinase(s) is involved in angiogenic endothelial cell proliferation, and that experiments involving erbstatin will provide an important due to understand a mechanism of angiogenesis.
Oikawa
T
T
Division of Cancer Therapeutics, Tokyo Metropolitan Institute of Medical Science, Japan.
Ashino
H
H
Shimamura
M
M
Hasegawa
M
M
Morita
I
I
Murota
S
S
Ishizuka
M
M
Takeuchi
T
T
D000818:Animals; D002455:Cell Division / Q000187:drug effects; D002642:Chick Embryo; D004305:Dose-Response Relationship, Drug; D006873:Hydroquinones / Q000494:pharmacology*; D009389:Neovascularization, Pathologic / Q000517:prevention & control*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*
D006873:Hydroquinones; D011505:Protein-Tyrosine Kinases; C048212:erbstatin