Structural biologists are deciphering the mechanisms of complex biological processes at a breathtaking pace. X-ray crystallography is providing atomic-resolution structures of complex molecular assemblies, and NMR spectroscopy is providing structural and dynamical information for ever-larger biomolecules in solution and in membranes. Fluorescence spectroscopy is yielding images of macromolecular machines at work both in vitro and in vivo. This wealth of structural information is complemented by dramatic improvements in the computational analysis of the structure and dynamics of biological macromolecules. The integration of all this new information requires an inter-disciplinary approach that utilizes a wide range of biochemical and biophysical tools to probe molecular function, while keeping the biologically important questions at center stage. The Keystone Meeting will bring together structural biologists interested in these issues, which have important implications both for fundamental biology and for the process of drug discovery.