ANTAGONISTIC EFFECT OF TRIPHENYLETHYLENIC ANTIESTROGENS ON THE ASSOCIATION OF ESTROGEN-RECEPTOR TO CALMODULIN

被引：43

作者：

BOUHOUTE, A ^{[1
]}

LECLERCQ, G ^{[1
]}

机构：

[1] INST JULES BORDET, SERV MED, LAB JC HEUSON CANCEROL MAMMAIRE & ENDOCRINOL, B-1000 BRUSSELS, BELGIUM

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1992年 / 184卷 / 03期

关键词：

D O I：

10.1016/S0006-291X(05)80043-9

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：

Binding of (3H)-estradiol labeled estrogen receptor from uterine cytosol to calmodulin was demonstrated by both affinity chromatography and sucrose gradient sedimentation. Triphenylethylene antiestrogens (tamoxifen family) with strong antagonistic activity against the calmodulin-dependent c-AMP phosphodiesterase largely reduced the binding of the receptor. Relevance of this observation with regard to the major antiproliferative activity (cytotoxicity) of these drugs is discussed. © 1992 Academic Press, Inc.

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页码：1432 / 1440

页数：9

相关论文

共 17 条

[1] THE ANTIPROLIFERATIVE EFFECT OF TAMOXIFEN IN BREAST-CANCER CELLS - MEDIATION BY THE ESTROGEN-RECEPTOR [J].

BARDON, S ;

VIGNON, F ;

DEROCQ, D ;

ROCHEFORT, H .

MOLECULAR AND CELLULAR ENDOCRINOLOGY, 1984, 35 (2-3) :89-96

[2] EFFECT OF TRIPHENYLACRYLONITRILE DERIVATIVES ON ESTRADIOL-RECEPTOR BINDING AND ON HUMAN-BREAST CANCER CELL-GROWTH [J].

BIGNON, E ;

PONS, M ;

DEPAULET, AC ;

DORE, JC ;

GILBERT, J ;

ABECASSIS, J ;

MIQUEL, JF ;

OJASOO, T ;

RAYNAUD, JP .

JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (09) :2092-2103

[3] INVITRO INTERACTION OF ESTRADIOL-RECEPTOR WITH CA-2+-CALMODULIN [J].

CASTORIA, G ;

MIGLIACCIO, A ;

NOLA, E ;

AURICCHIO, F .

MOLECULAR ENDOCRINOLOGY, 1988, 2 (02) :167-174

[4]

Celeste M, 1990, CANCER RES, V50, P2753

[5] ESTROGENIC AND ANTIESTROGENIC DOWN-REGULATION OF ESTROGEN-RECEPTOR LEVELS - EVIDENCE FOR 2 DIFFERENT MECHANISMS [J].

GYLING, M ;

LECLERCQ, G ;

HEUSON, JC .

JOURNAL OF RECEPTOR RESEARCH, 1990, 10 (5-6) :217-234

[6] IMPORTANCE OF THE ALKYLAMINOETHOXY SIDE-CHAIN FOR THE ESTROGENIC AND ANTI-ESTROGENIC ACTIONS OF TAMOXIFEN AND TRIOXIFENE IN THE IMMATURE RAT UTERUS [J].

JORDAN, VC ;

GOSDEN, B .

MOLECULAR AND CELLULAR ENDOCRINOLOGY, 1982, 27 (03) :291-306

[7] LOCALIZATION OF THE ESTRADIOL-BINDING AND PUTATIVE DNA-BINDING DOMAINS OF THE HUMAN ESTROGEN-RECEPTOR [J].

KUMAR, V ;

GREEN, S ;

STAUB, A ;

CHAMBON, P .

EMBO JOURNAL, 1986, 5 (09) :2231-2236

[8]

LECLERCQ G, 1992, IN PRESS J STEROID B

[9]

LIPPMAN M, 1976, CANCER RES, V36, P4595

[10] BINDING OF ANTIESTROGENS EXPOSES AN OCCULT ANTIGENIC DETERMINANT IN THE HUMAN ESTROGEN-RECEPTOR [J].

MARTIN, PM ;

BERTHOIS, Y ;

JENSEN, EV .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1988, 85 (08) :2533-2537