Circumventing tamoxifen resistance in breast cancers using antiestrogens that induce unique conformational changes in the estrogen receptor

Cancer Research

Volumn 61, Issue 7, 2001, Pages 2917-2922

  Connor, Caroline E ^a   Norris, John D ^a   Broadwater, Gloria ^a   Willson, Timothy M ^b   Gottardis, Marco M ^c   Dewhirst, Mark W ^a   McDonnell, Donald P ^a  

^a DUKE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b GLAXOSMITHKLINE   (United States)

^c BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (1,2 DIPHENYL 1 BUTENYL)CINNAMIC ACID; 4 HYDROXYTAMOXIFEN; ANTIESTROGEN; ESTRADIOL; ESTROGEN RECEPTOR; FULVESTRANT; GW 7604; IDOXIFENE; RALOXIFENE; TAMOXIFEN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BREAST CANCER; CELL TYPE; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; CROSS RESISTANCE; FEMALE; HORMONE RECEPTOR INTERACTION; HUMAN; HUMAN CELL; MOUSE; NONHUMAN; PHAGE DISPLAY; PRIORITY JOURNAL; TRANSCRIPTION REGULATION;

AMINO ACID SEQUENCE; ANIMALS; BREAST NEOPLASMS; CELL DIVISION; CINNAMATES; DRUG INTERACTIONS; DRUG RESISTANCE, NEOPLASM; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; ESTROGEN RECEPTOR MODULATORS; FEMALE; HUMANS; MICE; MICE, INBRED BALB C; MICE, NUDE; MOLECULAR SEQUENCE DATA; NEOPLASMS, HORMONE-DEPENDENT; PROTEIN CONFORMATION; RECEPTORS, ESTROGEN; STILBENES; TAMOXIFEN; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 0035300412     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (45)

1. Overviews of adjuvant tamoxifen therapy
2. The strategic use of antiestrogen to control the development and growth of breast cancer
3. Tamoxifen for adjuvant therapy and for the treatment of advanced disease in premenopausal breast cancer patients
4. A mono-hydroxylated metabolite of tamoxifen with potent antioestrogen activity
5. Why tamoxifen?
6. How is tamoxifen's action subverted?
7. Possible mechanisms in the emergence of tamoxifen-resistant breast cancer
8. Contrasting actions of tamoxifen on endometrial and breast tumor growth in the athymic mouse
9. Effects of tamoxifen on uterus
10. Effects of tamoxifen on cardiovascular risk factors in postmenopausal women
11. Effects of tamoxifen on bone mineral density in postmenopausal women with breast cancer
12. Tamoxifen withdrawal response. Report of a case
13. Molecular basis of agonism and antagonism in the oestrogen receptor
14. The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen
15. Estrogen receptor (ER) modulators each induce distinct conformational changes in ERα and ERβ
16. Peptide antagonists of the human estrogen receptor
17. Coactivator and corepressor regulation of the agonist/antagonist activity of the mixed antiestrogen, 4-hydroxytamoxifen
18. Diverse signaling pathways modulate nuclear receptor recruitment of N-CoR and SMRT complexes
19. Dissection of the LXXLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries: Discovery of peptide antagonists of estrogen receptors α and β
20. Development of tamoxifen-stimulated growth of MCF-7 tumors in athymic mice alter long-term antiestrogen administration
21. The novel anti-oestrogen idoxifene inhibits the growth of human MCF-7 breast cancer xenografts and reduces the frequency of acquired anti-oestrogen resistance
22. Dissection of the molecular mechanism of action of GW5638, a novel estrogen receptor ligand, provides insights into the role of ER in bone
23. Homologs of idoxifene: Variation of estrogen receptor binding and calmodulin antagonism with chain length
24. Tamoxifen is a calmodulin antagonist in the activation of cAMP phosphodiesterase
25. Inhibition of tamoxifen-stimulated growth of an MCF-7 tumor variant in athymic mice by novel steroidal antiestrogens
26. Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens
27. Comparative analyses of the mechanistic differences among antiestrogens
28. Acquired tamoxifen resistance: Correlation with reduced breast tumor levels of tamoxifen and isomerization of trans-4-hydroxytamoxifen
29. When tamoxifen turns bad
30. Human estrogen receptor transactivational capacity is determined by both cellular and promoter context and mediated by two functionally distinct intramolecular regions
31. The molecular pharmacology of SERMs
32. Definition of the cellular mechanisms which distinguish between hormone and antihormone activated steroid receptors
33. Yeast RSP5 and its human homologue hRPF1 potentiate hormone-dependent activation of transcription by human progesterone and glucocorticoid receptors
34. Antiproliferative and antiestrogenic effects of ICI 164, 384 and ICI 182, 780 in 4-OH tamoxifen-resistant human breast-cancer cells
35. Response to a specific antiestrogen (ICI182, 780) in tamoxifen-resistant breast cancer
36. Action of "pure" antiestrogens in inhibiting estrogen receptor action
37. Reproductive endocrine and endometrial effects of raloxifene hydrochloride, a selective estrogen receptor modulator, in women with regular menstrual cycles
38. Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women
39. Effects of high dose raloxifene in selected patients with advanced breast carcinoma
40. Comparison of the effects of a pure steroidal antiestrogen with those of tamoxifen in a model of human breast cancer
41. Nuclear receptor coregulators: Cellular and molecular biology
42. A signature motif in transcriptional co-activators mediates binding to nuclear receptors
43. Selective estrogen receptor modulators (SERMs): Research roundup
44. New endocrine therapies for breast cancer
45. Estrogen deprivation causes estradiol hypersensitivity in human breast cancer cells