THE ANTISTEROID RU486 - ITS CELLULAR AND MOLECULAR-MODE OF ACTION

被引：73
作者：
BAULIEU, EE
机构：
[1] Hormone Laboratory, INSERM U33
来源：
TRENDS IN ENDOCRINOLOGY AND METABOLISM | 1991年 / 2卷 / 06期
关键词：
D O I：
10.1016/1043-2760(91)90030-Q
中图分类号：
R5 [内科学];
学科分类号：
1002 ; 100201 ;
摘要：
RU486 is a very powerful antisteroid hormone compound, with antiprogestin and antiglucocorticosteroid clinical applications. High-affinity binding to the receptor ligand-binding domain results in essentially antagonistic function; however, some agonistlike effects have been observed. This review discusses the implications of recent discoveries concerning hsp90 (heat-shock protein M(r) approximately 90,000)-receptor interaction, receptor-DNA binding, and the involvement of transcription factors in the mechanism of action of RU486.
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页码：233 / 239
页数：7
相关论文
共 24 条
[11]   ANTIGLUCOCORTICOSTEROID EFFECTS SUGGEST WHY STEROID-HORMONE IS REQUIRED FOR RECEPTORS TO BIND DNA INVIVO BUT NOT INVITRO [J].
GROYER, A ;
SCHWEIZERGROYER, G ;
CADEPOND, F ;
MARILLER, M ;
BAULIEU, EE .
NATURE, 1987, 328 (6131) :624-626
[12]   RECEPTORS BOUND TO ANTIPROGESTIN FORM ABORTIVE COMPLEXES WITH HORMONE RESPONSIVE ELEMENTS [J].
GUIOCHONMANTEL, A ;
LOOSFELT, H ;
RAGOT, T ;
BAILLY, A ;
ATGER, M ;
MISRAHI, M ;
PERRICAUDET, M ;
MILGROM, E .
NATURE, 1988, 336 (6200) :695-698
[13]   Regulation of gene expression by nuclear hormone receptors [J].
Ham, J. ;
Parker, M. G. .
CURRENT OPINION IN CELL BIOLOGY, 1989, 1 (03) :503-511
[14]  
HERRMANN W, 1982, CR ACAD SCI III-VIE, V294, P933
[15]   FUNCTIONAL DOMAINS OF THE HUMAN ESTROGEN-RECEPTOR [J].
KUMAR, V ;
GREEN, S ;
STACK, G ;
BERRY, M ;
JIN, JR ;
CHAMBON, P .
CELL, 1987, 51 (06) :941-951
[16]   THE ESTROGEN-RECEPTOR BINDS TIGHTLY TO ITS RESPONSIVE ELEMENT AS A LIGAND-INDUCED HOMODIMER [J].
KUMAR, V ;
CHAMBON, P .
CELL, 1988, 55 (01) :145-156
[17]   AGONISTIC AND ANTAGONISTIC ACTIVITIES OF RU486 ON THE FUNCTIONS OF THE HUMAN PROGESTERONE-RECEPTOR [J].
MEYER, ME ;
PORNON, A ;
JI, JW ;
BOCQUEL, MT ;
CHAMBON, P ;
GRONEMEYER, H .
EMBO JOURNAL, 1990, 9 (12) :3923-3932
[18]   A SINGLE-STRANDED DNA-BINDING PROTEIN PROMOTES THE BINDING OF THE PURIFIED ESTROGEN-RECEPTOR TO ITS RESPONSIVE ELEMENT [J].
MUKHERJEE, R ;
CHAMBON, P .
NUCLEIC ACIDS RESEARCH, 1990, 18 (19) :5713-5716
[19]  
Philibert D., 1984, ADRENAL STEROID ANTA, P77
[20]   SEQUENCE-SPECIFIC POSITIONING OF NUCLEOSOMES OVER THE STEROID-INDUCIBLE MMTV PROMOTER [J].
RICHARDFOY, H ;
HAGER, GL .
EMBO JOURNAL, 1987, 6 (08) :2321-2328
123