X-Ray Crystallography of Agonist/Antagonist-Bound Receptors

Crystallographic analysis of the ligand-binding domains of nuclear hormone receptors (NR) has provided a unique insight into the molecular events that underlie the ligand-mediated control of their transcriptional activity. The technique relies on preparing milligram quantities of protein, growing three-dimensional crystals of the desired protein—ligand complex, collecting X-ray diffraction data, and subsequently interpreting the derived electron density maps to reveal the structure of the complex.