Perimenopausal and postmenopausal hormone replacement therapy Part 1. An update of the literature on benefits and risks*1

Lichtman, Ronnie

doi:10.1016/0091-2182(95)00082-8

Cited by 31 publications

(28 citation statements)

References 279 publications

(315 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…To alleviate or prevent symptoms of the nature described above and the development of serious health risks, women are given estrogen replacement therapy in combination with a gestagen (Lichtman, 1996). However, current hormone replacement therapy is associated with certain serious concerns like fear for increased risk of breast or uterine cancer, indicating the need for development of safer therapy.…”

mentioning

confidence: 97%

“…Furthermore, women may experience serious health risks such as the development of osteoporosis or cardiovascular disease during their postmenopausal life (Lichtman, 1996). The symptoms and health risks affecting many menopausal/postmenopausal women have been attributed to the loss of de novo production of the natural female sex hormone E2 (i.e., to an E2-deficient state).…”

mentioning

confidence: 99%

See 1 more Smart Citation

Differential Response of Estrogen Receptor α and Estrogen Receptor β to Partial Estrogen Agonists/Antagonists

et al. 1998

View full text Add to dashboard Cite

The existence of two rather than one estrogen receptor, today characterized as estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta), indicates that the mechanism of action of 17beta-estradiol and related synthetic drugs is more complex than previously thought. Because the homology of amino acid residues in the ligand-binding domain (LBD) of ERbeta is high compared with those amino acid residues in ERalpha LBD, previously shown to line the ligand binding cavity or to make direct contacts with ligands, it is not surprising that many ligands have a similar affinity for both receptor subtypes. We report that 17alpha-ethynyl, 17beta-estradiol, for example, has an ERalpha-selective agonist potency and that 16beta,17alpha-epiestriol has an ERbeta-selective agonist potency. We also report that genistein has an ERbeta-selective affinity and potency but an ERalpha-selective efficacy. Furthermore, we show that tamoxifen, 4-OH-tamoxifen, raloxifene, and ICI 164,384 have an ERalpha-selective partial agonist/antagonist function but a pure antagonist effect through ERbeta. In addition, raloxifene displayed an ERalpha-selective antagonist potency, in agreement with its ERalpha-selective affinity. However, although ICI 164,384 showed an ERbeta-selective affinity, it had a similar potency to antagonize the effect of 17beta-estradiol in the ERalpha- and ERbeta-specific reporter cell lines, respectively. In conclusion, our data indicate that the ligand binding cavity of ERbeta is probably more different from that of ERalpha than can be anticipated from the primary sequences of the two ER subtypes and that it will be possible to develop receptor-specific ligands that may form the basis of novel pharmaceuticals with better in vivo efficacy and side effect profile than current available drugs.

show abstract

mentioning

confidence: 97%

mentioning

confidence: 99%

Differential Response of Estrogen Receptor α and Estrogen Receptor β to Partial Estrogen Agonists/Antagonists

et al. 1998

View full text Add to dashboard Cite

show abstract

“…Estrogens are claimed to be effective in the treatment of urge incontinence in postmenopausal women (see [54,55] and references cited therein). It has recently been shown that ERβ is highly expressed in the inner epithelial cell layer of the rat bladder and urethra [56,57], which may explain the beneficial effect of estrogens in urinary incontinence and suggest that patients with urinary incontinence might benefit from ERβ-selective agonist therapy.…”

Section: Tissue Distribution Of Erbeta and Eralphamentioning

confidence: 99%

“…There is compelling evidence that estrogens protect post-menopausal women from bone loss and the development of osteoporosis, maintaining a balance between bone resorption and bone formation [54,55,60,61,62,63]. As in other tissues, estrogens probably have both direct and indirect effects in maintaining a balanced bone metabolism.…”

Section: Tissue Distribution Of Erbeta and Eralphamentioning

confidence: 99%

See 1 more Smart Citation

Estrogen receptor transcription and transactivation Basic aspects of estrogen action

2000

View full text Add to dashboard Cite

Estrogen signaling has turned out to be much more complex and exciting than previously thought; the paradigm shift in our understanding of estrogen action came in 1996, when the presence of a new estrogen receptor (ER), ERβ, was reported. An intricate interplay between the classical ERα and the novel ERβ is of paramount importance for the final biological effect of estrogen in different target cells.

show abstract

Sexuality After Hematopoietic Cell Transplantation

Tierney¹

2003

Thomas' Hematopoietic Cell Transplantation

View full text Add to dashboard Cite

Perimenopausal and postmenopausal hormone replacement therapy Part 1. An update of the literature on benefits and risks*1

Cited by 31 publications

References 279 publications

Differential Response of Estrogen Receptor α and Estrogen Receptor β to Partial Estrogen Agonists/Antagonists

Differential Response of Estrogen Receptor α and Estrogen Receptor β to Partial Estrogen Agonists/Antagonists

Estrogen receptor transcription and transactivation Basic aspects of estrogen action

Sexuality After Hematopoietic Cell Transplantation

Contact Info

Product

Resources

About