Effective Use of Selective Estrogen Receptor Modulators

A Science Daily article titled Moving Beyond Tamoxifen: Drug Discovery And The Future Of Selective Hormone Receptor Modulators discusses the potential benefits that could accrue from further development of a class of drugs described by the term selective estrogen receptor modulators. SERMs come in different varieties and have strikingly different effects on different cell types as the word selective infers. As the linked article notes SERMs can mimick the effects of estrogen at one location while causing quite different outcomes at another.

The variation of effects produced by SERMs can be explained by the nature of estrogen receptors and gene expression dynamics. There is variation among receptors. When bonding with a recptor occurs a cascade of biochemical reactions can follow determining which genes will be expressed and which will not be.

The Science Daily article specifically mentions a SERM known as raloxifene which can have anti-carcinogenic effects through anti-estrogen activity in breast tissue. However, raloxifene can also promote increased bone density in other tissue through estrogen-like effects.