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5. Molecular design of auxin antagonists specific to TIR1/AFB auxin receptors
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- Hirose Masakazu
- Dept. of Biochemistry, Okayama Univ. of Science
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- kepinski Stefan
- Centre for Plant Sciences, Leeds Univ.
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- Shimada Yukihisa
- RIKEN, PSC
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- Nozaki Hiroshi
- Dept. of Biochemistry, Okayama Univ. of Science
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- Hayashi Ken-ichiro
- Dept. of Biochemistry, Okayama Univ. of Science
Bibliographic Information
- Other Title
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- 5.TIR1/AFBオーキシン受容体特異的拮抗剤の分子設計(口頭発表)
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Description
TIR1/AFB auxin receptors play a central role in the perception of auxin and regulate the many aspects of auxin-regulated developmental processes in plant. Therefore, specific auxin antagonists on TIR1/AFB receptors are promising chemical tools for auxin biology. We have found that α-alkyl-IAA function as specific auxin antagonists to block TIR1/AFB function. Our efforts for the development of new potent auxin antagonists using virtual screening and structure-based drug design lead to the identification of potent lead compounds, PEO-IAA that showed a high affinity to TIR1 and anti-auxin activities in planta. We then optimized the structure of PEO-IAA to show higher auxin antagonistic activity. As the results of derivatization, mXO-IAA, new antagonistic probe exhibited potent and specific inhibitory activity on SCF (TIR1) signaling.
Journal
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- The Janapese Society for Chemical Regulation of Plants, Abstract
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The Janapese Society for Chemical Regulation of Plants, Abstract 45 (0), 22-, 2010
The Janapese Society for Chemical Regulation of Plants
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Details 詳細情報について
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- CRID
- 1390282679399174144
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- NII Article ID
- 110007767105
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- ISSN
- 21896313
- 09191887
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- Text Lang
- ja
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- Data Source
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- JaLC
- CiNii Articles
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- Abstract License Flag
- Disallowed