Selective estrogen receptor modulators: Mechanism of action and clinical experience. Focus on raloxifene

Reproduction, Fertility and Development

Volumn 13, Issue 4, 2001, Pages 331-336

  Thiebaud, D ^a   Secrest, R J ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,1,2 TRIPHENYLETHYLENE DERIVATIVE; BENZOTHIOPHENE; CLOMIFENE; ESTROGEN RECEPTOR; LIPID; PLACEBO; RALOXIFENE; RECEPTOR BLOCKING AGENT; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN; TOREMIFENE;

AGONIST; BIOLOGY; BONE DENSITY; BREAST; CLINICAL TRIAL; COMPLEX FORMATION; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG MECHANISM; DRUG RECEPTOR BINDING; ESTROGEN ACTIVITY; EXPERIENCE; FEMALE; HUMAN; LIGAND BINDING; LIPID BLOOD LEVEL; MAJOR CLINICAL STUDY; PROTEIN STRUCTURE; RANDOMIZED CONTROLLED TRIAL; REVIEW; TARGET ORGAN; TISSUE SPECIFICITY; UTERUS; VASCULARIZATION;

CLINICAL TRIALS; FEMALE; HUMANS; RALOXIFENE; RECEPTORS, ESTROGEN; SELECTIVE ESTROGEN RECEPTOR MODULATORS;

EID: 0035211987     PISSN: 10313613     EISSN: None     Source Type: Journal    
DOI: 10.1071/RD00109     Document Type: Review

References (43)

1. The potential of SERMs for reducing the risk of coronary heart disease
2. Molecular basis of agonism and antagonism in the oestrogen receptor
3. Characterization of hot flashes reported by healthy postmenopausal women receiving raloxifene or placebo during osteoporosis prevention trials
4. Tissue distribution and quantitative analysis of estrogen receptor-alpha (ERalpha) and estrogen receptor-beta (ERbeta) messenger ribonucleic acid in the wild-type and ERalpha-knockout mouse
5. The effect of raloxifene on risk of breast cancer in postmenopausal women
6. Identification of a conserved region required for hormone dependent transcriptional activation by steroid hormone receptors
7. Adverse events reported by postmenopausal women in controlled trials with raloxifene
8. Estrogen and estrogen receptor antagonists stimulate transcription from the human retinoic acid receptor-α-1 promoter via a novel sequence
9. Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: Results from a 3-year randomized clinical trial
10. The steroid and thyroid hormone receptor superfamily
11. Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear receptors
12. Endometrial cancer in tamoxifen-treated breast cancer patients: Findings from the National Surgical Adjuvant Breast and Bowel Project (NSABP) B-14
13. Markers of bone resorption predict hip fracture in elderly women: The EPIDOS prospective study
14. Estrogen receptor β: Re-evaluation of estrogen and antiestrogen signaling
15. Structural and functional domains of the estrogen receptor
16. Randomized trial of estrogen plus progestin for secondary prevention of coronary heart disease in postmenopausal women
17. Risk of hospital admission for idiopathic venous thromboembolism among users of postmenopausal oestrogens
18. Tamoxifen, raloxifene, and the prevention of breast cancer
19. Hypocholesterolemic activity of raloxifene (LY139481): Pharmacological characterization as a selective estrogen receptor modulator
20. The novel estrogen receptor-beta subtype: Potential role in the cell- and promoter-specific actions of estrogens and anti-estrogens
21. Cloning of a novel estrogen receptor expressed in rat prostate and ovary
22. Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta
23. The estrogen receptor beta subtype: A novel mediator of estrogen action in neuroendocrine systems
24. The Molecular Pharmacology of SERMs
25. Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens
26. Relationship of bone turnover to bone density and fractures
27. Treatment of postmenopausal women with osteoporosis or low bone density with raloxifene
28. Selective estrogen receptor modulators: A look ahead
29. Human estrogen receptor ligand activity inversion mutants: Receptors that interpret antiestrogens as estrogens and estrogens as antiestrogens and discriminate among different antiestrogens
30. An estrogen receptor-selective coregulator that potentiates the effectiveness of antiestrogens and represses the activity of estrogens
31. ER beta: Identification and characterization of a novel human estrogen receptor
32. Identification of a third autonomous activation domain within the human estrogen receptor
33. Differential ligand activation of estrogen receptors ERalpha and ERbeta at AP1 sites
34. Estrogen receptor (ER) modulators each induce distinct conformational changes in ER alpha and ER beta
35. Effects of raloxifene and hormone replacement therapy on homocysteine and C-reactive protein levels in postmenopausal women
36. Estrogen receptors in the rat uterus. Studies on the interaction of cytosol and nuclear binding sites
37. Selective estrogen receptor modulators
38. Molecular mechanisms of action of steroid/thyroid receptor superfamily members
39. Human estrogen receptor transactivational capacity is determined by both cellular and promoter context and mediated by two functionally distinct intramolecular regions
40. Effects of raloxifene on serum lipids and coagulation factors in healthy postmenopausal women
41. The Effects of hormone replacement therapy and raloxifene on C-reactive protein and homocysteine in healthy postmenopausal women: A randomized, controlled trial
42. Estrogen and raloxifene stimulate transforming growth factor-β3 gene expression in rat bone: A potential mechanism for estrogen- or raloxifene-mediated bone maintenance
43. Identification of an estrogen response element activated by metabolites of 17beta-estradiol and raloxifene