The nuclear hormone receptors engender great research interest, and have spawned numerous scientific meetings. The past Keystone Symposia dealt with this topic from the perspective of molecular biology. This meeting will bring together three aspects of research impacting human heath via the nuclear receptors. These three groups are (a) basic scientists, (b) pharmaceutical drug discoverers and (c) clinicians. The meeting will unfold a series of questions regarding unmet medical needs for drugs involving nuclear receptor ligands, recent advances towards a molecular understanding of tissue-selectivity as a hallmark for improved safety and efficacy, and a resources workshop to address and fulfill needs for emerging novel research tools. This meeting will differ from other Keystone meetings dealing with the nuclear hormone receptor family by concentrating upon the link of molecular tools to unmet medical needs for improved therapeutics.