NONSTEROIDAL ANTIESTROGEN SUPPRESSES PROTEIN-KINASE-C - ITS INHIBITORY EFFECT ON INTERACTION OF SUBSTRATE PROTEIN WITH MEMBRANE

被引：17

作者：

EDASHIGE, K

SATO, EF

AKIMARU, K

YOSHIOKA, T

UTSUMI, K

机构：

[1] KOCHI MED SCH, DEPT MED BIOL, KOCHI 783, JAPAN

[2] KOCHI MED SCH, INST LAB ANIM, KOCHI 783, JAPAN

[3] CTR ADULT DIS, MED SCI LAB, KURASHIKI 710, JAPAN

来源：

CELL STRUCTURE AND FUNCTION | 1991年 / 16卷 / 04期

关键词：

PROTEIN KINASE-C; ANNEXIN; ANTIESTROGEN; MEMBRANE-PROTEIN INTERACTION;

D O I：

10.1247/csf.16.273

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

The mechanism by which nonsteroidal antiestrogen inhibits Ca2+- and phospholipid-dependent protein kinase (PKC) activity was investigated. Antiestrogenic agents, clomiphene and tamoxifen, inhibited the PKC-dependent phosphorylation of histone and r-annexin I in a dose-dependent manner. Ki values for the agents were different for two substrate proteins. The inhibitory action of the agents depended on the membrane-substrate protein interaction. Phosphorylation of cytoplasmic proteins obtained from rat uterus and mammary gland, including annexin I, by endogenous PKC was also inhibited by low concentrations of these agents. These results suggest that the inhibitory action of nonsteroidal antiestrogens occurs through their inhibitory effect on the membrane-substrate protein interaction.

引用

页码：273 / 281

页数：9

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