Twenty-five years of nuclear receptor structure analysis: From the laboratory to the clinic

High resolution structural analysis of nuclear receptors has been possible for the last twenty-five years. During this period we have moved from a schematic representation of nuclear receptors, based on biochemical studies, to crystal and NMR structures of the isolated ligand binding and DNA binding domains, which have increased our understanding of receptor structure and provided fresh insights into function. Recent progress has seen the emergence of almost complete three-dimensional descriptions for nuclear receptor complexes bound to cognate response elements. These dramatic advances in structural analysis are paralleled by the growing evidence linking nuclear receptor function to normal physiological processes and disease. The insights gained from nuclear receptor structures have the potential to be translated into new drugs for major diseases, including cancer, metabolic syndrome and cardiovascular disease