MECHANISMS OF ANTIHORMONE ACTION

被引：93

作者：

GRONEMEYER, H ^{[1
]}

BENHAMOU, B ^{[1
]}

BERRY, M ^{[1
]}

BOCQUEL, MT ^{[1
]}

GOFFLO, D ^{[1
]}

GARCIA, T ^{[1
]}

LEROUGE, T ^{[1
]}

METZGER, D ^{[1
]}

MEYER, ME ^{[1
]}

TORA, L ^{[1
]}

VERGEZAC, A ^{[1
]}

CHAMBON, P ^{[1
]}

机构：

[1] ROUSSEL UCLAF,CTR RECH,DEPT ENDOCRINOL,F-93230 ROMAINVILLE,FRANCE

来源：

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY | 1992年 / 41卷 / 3-8期

关键词：

D O I：

10.1016/0960-0760(92)90347-L

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：

The mechanisms of action of two types of antihormones is discussed. Type I antihormones comprise the antiestrogen hydroxy-tamoxifen and the antiprogestin RU486, both of which promote DNA binding of the cognate receptors and, due to the activity of one of the two transcription activation functions of the estrogen and progesterone receptors, act as mixed agonist/antagonists. Evidence supporting that ICI 164,384 is also a member of the same group is presented. Type II antagonists impair DNA binding of the corresponding receptor in vitro and, in some cases, also in vivo. Ligand-mapping, an approach to identify the site of interaction of a steroid substitution within the hormone-binding domain of the receptor has been used to identify the 11-beta-pocket of the progesterone receptor and revealed that a single amino acid is responsible for the differential antagonistic effect of RU486 in man, chicken and hamster.

引用

页码：217 / 221

页数：5

共 36 条

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