Interaction of chemopreventive agents with hormone receptors.

Our understanding of the mechanisms by which chemopreventive agents interact with hormone receptors is clearly important both to current strategies for the treatment and prevention of cancer and to future endeavours of rational drug design, perhaps aided by computer-based molecular modelling. This chapter focuses on the importance of the interaction of the nonsteroidal antiestrogen drug tamoxifen (widely used in the treatment of breast cancer and currently being proposed for the prevention of breast cancer) with the estrogen receptor to its mode of action. The improved efficacy of new tamoxifen derivatives and of the steroidal pure estrogen antagonists is also considered, and the importance of hormone-receptor mutations in the development of drug resistance in cancer cells is discussed.