Invention of superagonists and superantagonists for ORL1 nociceptin receptor
| Project/Area Number |
23657078
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Structural biochemistry
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| Research Institution | Kyushu University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
MATSUSHIMA Ayami 九州大学, 大学院・理学研究院, 准教授 (60404050)
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| Project Period (FY) |
2011 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2012: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2011: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
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| Keywords | 分子認識 / 蛋白質 / 生理活性 / 脳・神経 / 鎮痛・疼痛 |
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| Research Abstract |
The principal objective of this project is to carry out so-called total Ala-scanning of ORL1 nociceptin receptor and then to identify the residues essential for the receptor activation. To date, the Ala-scanning was achieved with successful Ala-mutation of more than 247 scheduled-residues (270 in total), and further the more than 10 of amino acid residues were explored as essentials for the receptor activation. Eventually, we achieved the establishment in general molecular design of ligands that work for activity enhancement or suppression by bind or interfere specifically for these residues.
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Report
(3 results)
Research Products
(84 results)
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[Journal Article] Peptide Science 20112012
Author(s)
A. Matsushima, H. Nishimura, S. Inamine, S. Uemura, and Y. Shimohigashi
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Journal Title
Affinity labeling of the ORL1 nociceptin receptor by Cys(Npys)-elongated RYYRIK peptide antagonist
Volume: なし
Pages: 179-180
Related Report
Peer Reviewed
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[Presentation] Halogenation of Phe-phenyl in Opioid Peptide Engdomorphin-2 for Invention of Antagonist2012
Author(s)
Nishio, K., Nishimura, H., Suyama, K., Matsushima, A., Nose, T., and Shimohigashi, Y.
Organizer
16th Korean Peptide Protein Symposium
Place of Presentation
Sungkyunkwan University(成均館大學校)(Suwon水原市、韓国)
Year and Date
2012-11-30
Related Report
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[Presentation] Pharmacological chaperone for fine protein expression of orl1 nociceptin receptor in the cell membrane2012
Author(s)
Nishimura, H., Inamine, S., Li, J., Matsushima, A., and Shimohigashi, Y.
Organizer
16th Korean Peptide Protein Symposium
Place of Presentation
Sungkyunkwan University, Suwon, Korea
Related Report
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[Presentation] Halogenation of Phe-phenyl in Opioid Peptide Engdomorphin-2 for Invention of Antagonist2012
Author(s)
Nishio, K., Nishimura, H., Suyama, K., Matsushima, A., Nose, T., and Shimohigashi, Y.
Organizer
16th Korean Peptide Protein Symposium
Place of Presentation
Sungkyunkwan University, Suwon, Korea
Related Report
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