ABSTRACT
The usefulness of high-resolution protein structural data in the development of small-
molecule drugs is well established. In contrast, the role of structural information in the development of protein Pharmaceuticals may not initially be so apparent. This chapter describes the determination of the X-ray crystal structure of human interferon-β-la (IFNβ-1a), the active ingredient in Avonex®, the leading treatment worldwide for relapsing forms of multiple sclerosis. We review several ways in which this structure has been used to help address the biochemical and biological properties of this important cytokine and also its use in the design of second-generation drugs. In so doing, we illustrate some of the ways in which protein structure determination can be integrated with biochemical studies to elucidate the biochemical and biological properties of cytokines and how such work can have an impact on drug development in the biopharmaceutical industry.
