INHIBITION OF EPIDERMAL GROWTH FACTOR-INDUCED DNA-SYNTHESIS BY TYROSINE KINASE INHIBITORS

被引：157

作者：

UMEZAWA, K ^{[1
]}

HORI, T ^{[1
]}

TAJIMA, H ^{[1
]}

IMOTO, M ^{[1
]}

ISSHIKI, K ^{[1
]}

TAKEUCHI, T ^{[1
]}

机构：

[1] INST MICROBIAL CHEM,SHINAGAWA KU,TOKYO 141,JAPAN

来源：

FEBS LETTERS | 1990年 / 260卷 / 02期

关键词：

(Normal rat kidney cell); Cell cycle; DNA synthesis; Epidermal growth factor; Erbstatin;

D O I：

10.1016/0014-5793(90)80102-O

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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 μg ml. 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. © 1990.

引用

页码：198 / 200

页数：3

共 11 条

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