Moving beyond tamoxifen: Drug discovery and the future of selective hormone receptor ...(st cancer. The idea that SERMs co...),Health

The idea that SERMs could act like an estrogen in one place and an anti-estrogen in the other has created a new dimension in drug development, Jordan says. Now we can look at the design of these drugs and see how they can be applied to modulate other receptor sites throughout the body.

According to Jordan, recent studies have shown light on the complex and seemingly contradictory mechanisms behind the activity of receptors for steroids, such as estrogen. These mechanisms include slight structural differences in the estrogen receptors themselves in different tissues, as well as co-regulatory molecules that can influence whether a SERM will turn on or shut down a particular receptor. Of the 48 or so members of the nuclear receptor family, which include the molecules inside cells that bind to estrogen and other hormones, nearly half are able to be regulated in some way.

Our knowledge of how tamoxifen and raloxifene work is now being applied to develop new drugs that are selective male hormone receptor modulators that could be used in men to improve muscle weight during sickness, but without stimulating glands like the prostate, Jordan says. Indeed, a whole variety of nuclear steroid hormone receptor mediated drugs are now possible because of the understanding of SERM action.

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