Molecular mechanisms of selective estrogen receptor modulator (SERM) action.

Perspectives in Pharmacology Molecular Mechanisms of Selective Estrogen Receptor Modulator (SERM) Action

In females, estrogens play a key role in reproduction and have beneficial effects on the skeletal, cardiovascular, and central nervous systems. Most estrogenic responses are mediated by estrogen receptors (ERs), either ERa or ERb, which are members of the nuclear receptor superfamily of ligand-dependent transcription factors. Selective estrogen receptor modulators (SERMs) are ER ligands that in...

Reducing the Risk of Endometrial Cancer in Patients Receiving Selective Estrogen Receptor Modulator (SERM) Therapy

Estrogen receptor pathways to AP-1.

Estrogen receptor (ER) binds to estrogen response elements in target genes and recruits a coactivator complex of CBP-pl60 that mediates stimulation of transcription. ER also activates transcription at AP-1 sites that bind the Jun/Fos transcription factors, but not ER. We review the evidence regarding mechanisms whereby ER increases the activity of Jun/Fos and propose two pathways of ER action d...

Use of Preclinical and Early Clinical Data for Dose Selection of a Selective Estrogen Receptor Modulator Toremifene in Treatment of Breast Cancer

In development of human medicines, it is important to predict early and accurately enough the disease and patient population to be treated as well as the effective and safe dose range of the studied medicine. This is pursued by using preclinical research models, clinical pharmacology and early clinical studies with small sample sizes. When successful, this enables effective development of medic...

Comparison of the Inhibitory Effect of Gonadotropin Releasing Hormone (GnRH) Agonist, Selective Estrogen Receptor Modulator (SERM), Antiprogesterone on Myoma Cell Proliferation In Vitro

Uterine myomas are the most common gynecologic tumor in women of reproductive age. Treatment options of uterine myomas consist of surgical, medical and interventional therapy such as uterine artery embolization or myolysis. Given that it is the most common type of tumor in women of reproductive age, the treatment of uterine myomas must prioritize uterine conservation. There are several drugs fo...