2017 Fiscal Year Final Research Report
Differential analysis of the crystal structures of active / inactive orexin receptor contributing to rational development of sleep control drug
Project/Area Number |
15K08268
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
General medical chemistry
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Research Institution | Kyoto University |
Principal Investigator |
Suno Ryoji 京都大学, 医学研究科, 特定助教 (60447521)
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Co-Investigator(Kenkyū-buntansha) |
野村 紀通 京都大学, 医学研究科, 助教 (10314246)
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Co-Investigator(Renkei-kenkyūsha) |
KOBAYASHI Takuya 京都大学, 医学研究科, 准教授 (20311730)
Yanagisawa Masashi 筑波大学, 国際統合睡眠医科学研究機構, 教授 (20202369)
Saitoh Tsuyoshi 筑波大学, 国際統合睡眠医科学研究機構, 助教 (80609933)
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Research Collaborator |
Kobilka Brian K スタンフォード大学, 医学部, 教授
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Project Period (FY) |
2015-04-01 – 2018-03-31
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Keywords | ヒト膜受容体 / GPCR / シグナル伝達 / X線結晶構造解析 / 抗体 / 薬剤開発 / ナルコレプシー |
Outline of Final Research Achievements |
Our goal is to determine the active and inactive crystal structures of OX1R and OX2R. We determined the structure of the selective antagonist EMPA-bound OX2R, and revealed the molecular mechanism of the selectivity of EMPA in detail. As the three-dimensional structure of OX1R and OX2R became clear, it was possible to provide useful information for drug development based on structural information. In addition, various tertiary structure-recognizing antibodies can be obtained during the research period, and one of them has been a functional antibody that inhibits signal transduction up to now. In the future, structure determination of active OX2R is expected as a part of research aimed at developing therapeutic drug for narcolepsy.
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Free Research Field |
構造生物学
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