Targeting nuclear receptors: PPARs as targets for drug design

Nuclear receptors form a large superfamily of zinc finger domain DNA-binding transcription factors (Fig. 9.1). This family includes the receptors for steroidal sex hormones such as oestrogen, progesterone and testosterone and it is these sex hormone receptors that have previously been targeted heavily for drug development. The two most notable drugs of this category are steroid antagonists, i.e. tamoxifen and RU486. Tamoxifen is an oestrogen receptor antagonist used in the secondary prevention of breast cancer1 and RU486 is a progesterone receptor antagonist utilized in induction of parturition.2