Targeted anti-estrogens to treat and prevent diseases in women

被引:29
作者
Tonetti, DA
Jordan, VC
机构
[1] Dept. Molec. Pharmacol. Biol. Chem., Robert H. Lurie Cancer Center, NW University Medical School, Chicago, IL 60611
来源
MOLECULAR MEDICINE TODAY | 1996年 / 2卷 / 05期
关键词
D O I
10.1016/1357-4310(96)88775-2
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 estrogen receptor has been successfully targeted with the anti-estrogen tamoxifen to treat all stages of breast cancer. Because tamoxifen is a partial agonist, it exhibits target-site specificity: it acts as an anti-estrogen in the breast to inhibit tumor growth, while exhibiting estrogenic effects on bones and lipid metabolism. Therefore, tamoxifen has the added benefit of maintaining bone density and reducing the risk of myocardial infarction in postmenopausal women. However, undesirable side effects of tamoxifen preclude its use as a hormone replacement therapy for otherwise healthy women. New anti-estrogens are currently being developed that may prevent osteoporosis, breast and endometrial cancer, and reduce the risk of myocardial infarction.
引用
收藏
页码:218 / 223
页数:6
相关论文
共 37 条
[31]   FATAL MYOCARDIAL-INFARCTION IN THE SCOTTISH ADJUVANT TAMOXIFEN TRIAL [J].
MCDONALD, CC ;
STEWART, HJ .
BRITISH MEDICAL JOURNAL, 1991, 303 (6800) :435-437
[32]  
McGuire W.L., 1975, Estrogen Receptors in Human Breast Cancer
[33]   DROLOXIFENE, A NEW ANTIESTROGEN - ITS ROLE IN METASTATIC BREAST-CANCER [J].
RAUSCHNING, W ;
PRITCHARD, KI .
BREAST CANCER RESEARCH AND TREATMENT, 1994, 31 (01) :83-94
[34]   POSSIBLE MECHANISMS IN THE EMERGENCE OF TAMOXIFEN-RESISTANT BREAST-CANCER [J].
TONETTI, DA ;
JORDAN, VC .
ANTI-CANCER DRUGS, 1995, 6 (04) :498-507
[35]   HUMAN ESTROGEN-RECEPTOR TRANSACTIVATIONAL CAPACITY IS DETERMINED BY BOTH CELLULAR AND PROMOTER CONTEXT AND MEDIATED BY 2 FUNCTIONALLY DISTINCT INTRAMOLECULAR REGIONS [J].
TZUKERMAN, MT ;
ESTY, A ;
SANTISOMERE, D ;
DANIELIAN, P ;
PARKER, MG ;
STEIN, RB ;
PIKE, JW ;
MCDONNELL, DP .
MOLECULAR ENDOCRINOLOGY, 1994, 8 (01) :21-30
[36]   PROTECTIVE ACTIONS OF TAMOXIFEN AND 4-HYDROXYTAMOXIFEN AGAINST OXIDATIVE DAMAGE TO HUMAN LOW-DENSITY LIPOPROTEINS - A MECHANISM ACCOUNTING FOR THE CARDIOPROTECTIVE ACTION OF TAMOXIFEN [J].
WISEMAN, H ;
PAGANGA, G ;
RICEEVANS, C ;
HALLIWELL, B .
BIOCHEMICAL JOURNAL, 1993, 292 :635-638
[37]  
1992, LANCET, V339, P71