| Budget Amount *help |
¥19,240,000 (Direct Cost: ¥14,800,000、Indirect Cost: ¥4,440,000)
Fiscal Year 2015: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
Fiscal Year 2014: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
Fiscal Year 2013: ¥14,560,000 (Direct Cost: ¥11,200,000、Indirect Cost: ¥3,360,000)
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| Outline of Final Research Achievements |
X-ray crystallography offers an unprecedented opportunity to facilitate drug discovery. The structural information of the protein-ligand complex has the potential to find ways to improve the lead compounds. The best way is to determine the three dimensional structure of the complex by soaking the ligand in crystals. However, the soaking step has a problem because many lead compounds are low water-soluble. Such lead compounds must be dissolved in concentrated organic solvents, such as dimethyl sulfoxide (DMSO). We recently developed a new method for growing crystals in a high-strength hydrogel. This method enabled us to increase the mechanical stability of the crystals. In this study, we transferred the hydrogel-grown avidin/streptavidin or FABP crystals into a 50% DMSO solution containing the inhibitors. We observed the clear electron density maps of the compounds that are bound to the active sites.
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