| Budget Amount *help |
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Outline of Final Research Achievements |
In this study, the specific ligands and fluorescence probes for steroid hormone nuclear receptors were developed.
(1) Phthalazinone derivatives were developed as novel androgen antagonists, and acted as antagonists towards both wild-type and mutated ARs. As progesterone antagonists, compounds bearing a carborane or adamantane as the hydrophobic pharmacophore were developed.
(2) Coumarine derivatives were developed as fluorescent progesterone antagonists, whose fluorescence intensity was strongly increased by binding to progesterone receptor. Coumarine derivatives with androgen antagonistic activity were also developed.
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