FEBS Letters | |
Inhibition of epidermal growth factor‐induced DNA synthesis by tyrosine kinase inhibitors | |
Isshiki, Kunio2  Tajima, Hirohisa1  Takeuchi, Tomio2  Hori, Takashi1  Imoto, Masaya1  Umezawa, Kazuo1  | |
[1] Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223 Japan;Institute of Microbial Chemistry, 3-14-23 Kamiosaki, Shinagawa-ku. Tokyo 141, Japan | |
关键词: Erbstatin; Epidermal growth factor; DNA synthesis; Cell cycle; (Normal rat kidney cell); | |
DOI : 10.1016/0014-5793(90)80102-O | |
学科分类:生物化学/生物物理 | |
来源: John Wiley & Sons Ltd. | |
【 摘 要 】
We prepared methyl 2,5-dihydroxycinnamate as a stable analogue of erbstatin, a tyrosine kinase inhibitor. This analogue was about 4 times more stable than erbstatin in calf serum. It inhibited epidermal growth factor receptor-associated tyrosine kinase in vitro with an IC50 of 0.15 . It also inhibited in situ autophosphorylation of epidermal growth factor receptor in A431 cells. Methyl 2,5-dihydroxycinnamate was shown to delay the S-phase induction by epidermal growth factor in quiescent normal rat kidney cells, without affecting the total amount ofDNA synthesis. The effect of erbstatin on S-phase induction was smaller, possibly because of its shorter life time.
【 授权许可】
Unknown
【 预 览 】
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