Allosteric silencing of activating function 1 in the 4-hydroxytamoxifen estrogen receptor complex is induced by substituting glycine for aspartate at amino acid 351

Cancer Research

Volumn 60, Issue 18, 2000, Pages 5097-5105

  MacGregor Schafer, J ^a   Liu, H ^a   Bentrem, D J ^a   Zapf, J W ^a   Jordan, V C ^a  

^a NORTHWESTERN UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 HYDROXYTAMOXIFEN; 7ALPHA [9 (4,4,5,5,5 PENTAFLUOROPENTYLSULFINYL)NONYL]ESTRA 1,3,5(10) TRIENE 3,17BETA DIOL; ESTRADIOL; ESTROGEN RECEPTOR; TAMOXIFEN; TRANSFORMING GROWTH FACTOR ALPHA;

ALLOSTERISM; AMINO ACID SUBSTITUTION; ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CONTROLLED STUDY; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; LIGAND BINDING; PRIORITY JOURNAL; RECEPTOR AFFINITY; SITE DIRECTED MUTAGENESIS; STRUCTURE ACTIVITY RELATION;

ALLOSTERIC REGULATION; AMINO ACID SUBSTITUTION; ASPARTIC ACID; BINDING SITES; COMPARATIVE STUDY; DRUG INTERACTIONS; ESTRADIOL; ESTROGEN RECEPTOR MODULATORS; GLYCINE; HUMAN; KINETICS; LIGANDS; MUTAGENESIS, SITE-DIRECTED; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY; RALOXIFENE; RECEPTORS, ESTROGEN; RNA, MESSENGER; SUPPORT, NON-U.S. GOV'T; SUPPORT, U.S. GOV'T, NON-P.H.S.; SUPPORT, U.S. GOV'T, P.H.S.; TAMOXIFEN; TRANSFECTION; TRANSFORMING GROWTH FACTOR ALPHA; TUMOR CELLS, CULTURED;

EID: 0034665358     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. Tamoxifen for early breast cancer: An overview of the randomised trials
2. Tamoxifen for prevention of breast cancer: Report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study
3. Basic guide to the mechanisms of antiestrogen action
4. Development of tamoxifen-stimulated growth of MCF-7 tumors in athymic mice after long-term antiestrogen administration
5. Inhibition of tamoxifen-stimulated growth of an MCF-7 tumor variant in athymic mice by novel steroidal antiestrogens
6. Selective oestrogen receptor modulation: Molecular pharmacology for the millennium
7. A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity
8. Hydroxylated metabolites of tamoxifen are formed in vivo and bound to estrogen receptor in target tissues
9. Tamoxifen and metabolites in MCF-7 cells: Correlation between binding to estrogen receptor and cell growth inhibition
10. The human oestrogen receptor functions in yeast
11. Functional domains of the human estrogen receptor
12. Role of the two activating domains of the oestrogen receptor in the cell-type and promoter-context dependent agonistic activity of the anti-oestrogen 4-hydroxytamoxifen
13. Human estrogen receptor transactivational capacity is determined by both cellular and promoter context and mediated by two functionally distinct intramolecular regions
14. Ligand-dependent, transcriptionally productive association of the amino- and carboxyl-terminal regions of a steroid hormone nuclear receptor
15. Molecular basis of agonism and antagonism in the oestrogen receptor
16. The structural basis of estrogen receptor/co-activator recognition and the antagonism of this interaction by tamoxifen
17. Biochemical pharmacology of antiestrogen action
18. An estrogen receptor model to describe the regulation of prolactin synthesis by antiestrogens in vitro
19. Differences between estrogen- and antiestrogen-estrogen receptor complexes from human breast tumors identified with an antibody raised against the estrogen receptor
20. The estrogen receptor from a tamoxifen stimulated MCF-7 tumor variant contains a point mutation in the ligand binding domain
21. Estrogenic activity is increased for an antiestrogen by a natural mutation of the estrogen receptor
22. The key to the antiestrogenic mechanism of raloxifene is amino acid 351 (aspartate) in the estrogen receptor
23. Growth regulation of estrogen receptor negative breast cancer cells transfected with cDNAs for estrogen receptor
24. A naturally occurring estrogen receptor mutation results in increased estrogenicity of a tamoxifen analog
25. The interaction of raloxifene and the active metabolite of the antiestrogen EM-800 (SC 5705) with the human estrogen receptor
26. The oestrogen-like effect of 4-hydroxytamoxifen on induction of transforming growth factor α mRNA in MDA-MB-231 breast cancer cells stably expressing the oestrogen receptor
27. Peptide antagonists of the human estrogen receptor
28. Coactivator and corepressor regulation of the agonist/antagonist activity of the mixed antiestrogen, 4-hydroxytamoxifen
29. Sequence and characterization of a coactivator for the steroid hormone receptor superfamily
30. Estrogen receptor-associated proteins: Possible mediators of hormone-induced transcription
31. p300 Is a component of an estrogen receptor coactivator complex
32. Indolo[3,2-b]carbazole: A dietary-derived factor that exhibits both antiestrogenic and estrogenic activity
33. The human estrogen receptor has two independent nonacidic transcriptional activation functions
34. Human estrogen receptor regulation in a yeast model system and studies on receptor agonists and antagonists
35. Structure-function analysis of the hormone binding domain of the human estrogen receptor by region-specific mutagenesis and phenotypic screening in yeast
36. A model to describe how a point mutation of the estrogen receptor alters the structure-function relationship of antiestrogens
37. The stimulation of uterine complement component C3 gene expression by antiestrogens
38. Antagonism of estrogen- and antiestrogen-induced uterine complement component C3 expression by ICI 164,384
39. The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling
40. Identification of a third autonomous activation domain within the human estrogen receptor