Recent breakthroughs in the field of cryo-electron microcopy (cryo-EM) provide unprecedented prospects for determination of the structures of a variety of medically important macromolecular assemblies. Using new methods for image processing, we have now shown that protein structures can be resolved in atomic detail, at resolutions comparable to those achieved in high-resolution X-ray crystallography. In my lecture, I will discuss recent advances we have made in using cryo-EM to address selected problems in cancer biology and also review the broader context of the development of cryo-EM methods for studying protein complexes, viruses and cells as they relate to the development of improved therapeutic agents.