Abstract
One of the most costly steps in drug development is the identification of a genuinely druggable compound for human beings, from pre-clinical animal model research. In order to overcome this problem, the importance of screening compounds with desirable distributions and metabolism in human bodies, using a microdosing technique, is increasingly apparent. In addition, screening compounds with high ligand efficiency is crucial to identify druggable compounds at an early stage of the research, and structure-based drug development is the most powerful tool for this strategy. Thus, the combined utilization of structural biology/structural genomics and molecular imaging technology will be critically important for drug discovery research in the near future. This review focuses on current topics of structural genomics, including protein synthesis systems and structural analyses, toward rational drug development in collaboration with molecular imaging.
Keywords: Crystal, Histone, Inhibitor, Membrane protein, Nuclear magnetic resonance (NMR), X-ray structure.
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