2022 Fiscal Year Final Research Report
Development of an optochemical tool that regulate the intracellular synthesis of PPARgamma ligand
| Project/Area Number |
20K05742
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 37030:Chemical biology-related
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| Research Institution | University of Tsukuba |
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Principal Investigator |
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| Project Period (FY) |
2020-04-01 – 2023-03-31
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| Keywords | PPARγ / 核内受容体 / 生体直交化学 / 光化学 |
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| Outline of Final Research Achievements |
Peroxisome proliferator-activated receptor (PPAR) γ is a member of nuclear receptor superfamily, that regulates glucose and lipid metabolism. This study aimed to develop the methodology to facilitate the intracellular synthesis of PPARγ ligand through the light-irradiation by combining the bio-orthogonal chemistry and optochemistry. We synthesized a series of compounds that possess the reactive functional group but could not observe the intracellular ligation. We employed the alternative approach and successfully synthesize the PPARγ ligand that possess the photoreactive linker, which is expected as a new approach for light-control of PPARγ agonistic activity.
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| Free Research Field |
ケミカルバイオロジー
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| Academic Significance and Societal Importance of the Research Achievements |
本研究では、薬候補化合物の化学構造を細胞内で合成すること、また薬効の発現の有無を光照射により制御するための技術を開発することを目的とした。前者の目的については達成することが出来なかったが、後者については光反応性官能基を導入した化合物の合成に成功した。今後、光照射実験により得られた化合物の配座変化や薬効発現の制御を実証することで、新たな創薬技術の一つとなることが期待される。
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