Breast Cancer, Estrogen Receptor and Ligands

被引:102
作者
Bai, Zhenlin [1 ]
Gust, Ronald [1 ]
机构
[1] Free Univ Berlin, Inst Pharm, D-14195 Berlin, Germany
关键词
Anti-estrogen action; Breast cancer; Estrogen receptor; Ligand; Estrogen action; PROTEIN-COUPLED RECEPTOR; BASIC SIDE-CHAINS; HORMONE-BINDING GLOBULIN; GROWTH-FACTOR RECEPTOR; TRANSCRIPTIONAL ACTIVATION; MOLECULAR-MECHANISMS; BIOLOGICAL EVALUATION; MEMBRANE-RECEPTOR; PROMOTER-CONTEXT; ER ALPHA;
D O I
10.1002/ardp.200800174
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This review emphasizes the relationship of breast cancer, estrogen receptor and ligands, especially the centrality of the estrogen receptor, which mediates on one hand the hormone-induced gene transcription and on the other hand the anti-estrogen action against breast cancer. The characterization of the estrogen receptor ligand-binding domain co-crystallized with agonists or antagonists provided a molecular basis to gain an insight into the regulation of estrogen receptor and, thereby, to describe the mechanism of the hormone therapy in treating breast cancer.
引用
收藏
页码:133 / 149
页数:17
相关论文
共 135 条
[1]   Raloxifene [J].
Balfour, JA ;
Goa, KL .
DRUGS & AGING, 1998, 12 (04) :335-341
[2]  
Batzler W., 2008, Krebs in Deutschland 2003 - 2004. Haufigkeiten und Trends
[3]   TRANSCRIPTIONAL ACTIVATION BY THE ESTROGEN-RECEPTOR REQUIRES A CONFORMATIONAL CHANGE IN THE LIGAND-BINDING DOMAIN [J].
BEEKMAN, JM ;
ALLAN, GF ;
TSAI, SY ;
TSAI, MJ ;
OMALLEY, BW .
MOLECULAR ENDOCRINOLOGY, 1993, 7 (10) :1266-1274
[4]  
BENSDORF K, UNPUB
[5]   ROLE OF THE 2 ACTIVATING DOMAINS OF THE ESTROGEN-RECEPTOR IN THE CELL-TYPE AND PROMOTER-CONTEXT DEPENDENT AGONISTIC ACTIVITY OF THE ANTIESTROGEN 4-HYDROXYTAMOXIFEN [J].
BERRY, M ;
METZGER, D ;
CHAMBON, P .
EMBO JOURNAL, 1990, 9 (09) :2811-2818
[6]   CRYSTAL-STRUCTURE OF THE LIGAND-BINDING DOMAIN OF THE HUMAN NUCLEAR RECEPTOR RXR-ALPHA [J].
BOURGUET, W ;
RUFF, M ;
CHAMBON, P ;
GRONEMEYER, H ;
MORAS, D .
NATURE, 1995, 375 (6530) :377-382
[7]   EMERGING DIVERSITIES IN THE MECHANISM OF ACTION OF STEROID-HORMONES [J].
BRANN, DW ;
HENDRY, LB ;
MAHESH, VB .
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1995, 52 (02) :113-133
[8]   From ligand structure to biological activity: modified estratrienes and their estrogenic and antiestrogenic effects in MCF-7 cells [J].
Brooks, SC ;
Skafar, DF .
STEROIDS, 2004, 69 (06) :401-418
[9]   Correlation of aromatase and cyclooxygenase gene expression in human breast cancer specimens [J].
Brueggemeier, RW ;
Quinn, AL ;
Parrett, ML ;
Joarder, FS ;
Harris, RE ;
Robertson, FM .
CANCER LETTERS, 1999, 140 (1-2) :27-35
[10]   Molecular basis of agonism and antagonism in the oestrogen receptor [J].
Brzozowski, AM ;
Pike, ACW ;
Dauter, Z ;
Hubbard, RE ;
Bonn, T ;
Engstrom, O ;
Ohman, L ;
Greene, GL ;
Gustafsson, JA ;
Carlquist, M .
NATURE, 1997, 389 (6652) :753-758