Development of carrier molecule targeted GLUT
| Project/Area Number |
20K05755
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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 | Okayama University (2022)
Tokyo University of Science (2020-2021) |
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Principal Investigator |
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| Project Period (FY) |
2020-04-01 – 2023-03-31
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| Project Status |
Completed (Fiscal Year 2022)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2022: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2021: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2020: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
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| Keywords | ホウ素中性子線捕捉療法 / BSH / キャリア分子 / カチオン性ポリマー / ホウ素クラスター / ホウ素中性子線補足療法 / グルコーストランスポータ / 亜鉛錯体 / メディシナルケミストリー |
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| Outline of Research at the Start |
近年、がん治療の新たな選択肢の一つとしてホウ素中性子線捕捉療法（BNCT: Boron Neutron Capture Therapy）が注目されている。BNCTは10B化合物に中性子線を当てることによりα線を発生させることでその周囲の細胞を死滅させるものであるが、その実用化に向けての最も大きい課題は線源となりうる10B化合物を如何にしてがん細胞に集めるかということである。そこで、本研究課題ではがん細胞が独自の糖代謝系を有している事（ワールブルグ効果）に注目し、グルコーストランスポーターによってがん細胞に輸送され、配位結合によってBSHを担持可能なキャリア分子の創製研究を提案する。
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| Outline of Final Research Achievements |
In this research, we developed a technology to deliver BSH, which is used as a BNCT drug, into cells. The original plan was to develop carrier molecules that induce GLUT-mediated uptake, but we found that nanoparticles could be formed by mixing BSH with cationic polymers. Therefore, we decided to focus on these nanoparticles. When the cytotoxicity and cell membrane permeability of this nanoparticle were evaluated, it was revealed that the membrane permeability was significantly improved compared to BSH alone.
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| Academic Significance and Societal Importance of the Research Achievements |
BSHは構造中に複数のホウ素原子を有している事からBNCT用薬剤として有用であるにもかかわらず、その細胞膜透過性の低さからあまり使用されていない。本研究成果によってカチオン性ポリマーを混合するだけで、BSHの欠点である膜透過性を改善できたという点は今後のBNCT研究に大きく貢献するものである。
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Report
(4 results)
Research Products
(30 results)
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[Journal Article] Effect of N-Benzyl Group in Indole Scaffold of Thiosemicarbazones on the Biological Activity of Their Pd(II) Complexes: DFT, Biomolecular Interaction, in Silico Docking, ADME and Cytotoxicity Studies2022
Author(s)
Nithya Balakrishnan, Jebiti Haribabu, Rahime Eshaghimalekshah, Srividya Swaminathan, Chandrasekar Balachandran, Nattamai S.P. Bhuvanesh, Shin Aoki, Ramasamy Karvembu,
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Journal Title
Inorganica Chimica Acta
Volume: 534
Issue: 5
DOI
Related Report
Peer Reviewed
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[Journal Article] Isohamnetin Promotes 53BP1 Recruitment through the Enhancement of ATM Phosphorylation and Protects Mice from Radiation Gastrointestinal Syndrome2021
Author(s)
Yuichi Nishiyama, Akinori Morita, Shogo Tatsuta, Misaki Kanamaru, Masahiro Sakaue, Kenta Ueda, Manami Shono, Rie Fujita, Bing Wang, Yoshio Hosoi, Shin Aoki and Takeshi Sugai
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Journal Title
Genes
Volume: 12
Issue: 12
Pages: 8523-8544
DOI
Related Report
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[Journal Article] Crystal structures of fukutin-related protein (FKRP), a ribitol-phosphate transferase related to muscular dystrophy.2020
Author(s)
N. Kuwabara, R. Imae, H. Manya, T. Tanaka, M. Mizuno, H. Tsumoto, M. Kanagawa, K. Kobayashi, T. Toda, T. Senda, T. Endo & R. Kato
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Journal Title
Related Report
Peer Reviewed / Open Access
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[Presentation] Mefloquine Has a Potent Antiviral Activity against Severe Acute Respiratory Syndrome Related Coronavirus 22021
Author(s)
Kaho Shionoya, Masako Yamasaki, Shoya Iwanami, Yusuke Ito, Shuetsu Fukushi, Hirofumi Ohashi, Wakana Saso, Tomohiro Tanaka, Shin Aoki, Kouji Kuramochi, Shingo Iwami, Yoshimasa Takahashi, Tadaki Suzuki, Masamichi Muramatsu, Makoto Takeda, Takaji Wakita and Koichi Watashi
Organizer
第68回日本ウイルス学会学術学会
Related Report
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[Presentation] Design, Synthesis, and Antiviral Activity of Anti-SARS-CoV-2 Agents in Interdisciplinary Research2021
Author(s)
Haruka Uchiyama, Mayuka Nii, Tomohiro Tanaka, Kohei Akimoto, Hiroshi Takemura, Kaho Shionoya, Hirofumi Ohashi, Koichi Watashi, and Shin Aoki
Organizer
2020/2021 International Chemical Congress of Pacific Basin Societies (PACICHEM2020/2021)
Related Report
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