Development of anticancer therapy for urological malignancy using GGCT inhibitors
| Project/Area Number |
15K10584
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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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| Research Field |
Urology
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| Research Institution | Shiga University of Medical Science |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
富田 圭司 滋賀医科大学, 医学部, 助教 (30640148)
花田 英紀 滋賀医科大学, 医学部, 助教 (40555067)
吉田 哲也 滋賀医科大学, 医学部, 助教 (60510310)
平竹 潤 京都大学, 化学研究所, 教授 (80199075)
吉貴 達寛 滋賀医科大学, 医学部, 准教授 (80230704)
河内 明宏 滋賀医科大学, 医学部, 教授 (90240952)
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2017: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2016: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2015: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | γ-グルタミルシクロトランスフェラーゼ / 低分子化合物 / 抗癌剤 / 低分子阻害薬 / 抗がん剤 / 細胞老化 |
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| Outline of Final Research Achievements |
GGCT (gamma-glutamylcyclotransferase) is known to be one of cancer-promoting proteins. In this study we planned developing the low molecular compounds that can inhibit GGCT function in cancer proliferation. Among the 40 compounds we designed, GA (N-glutaryl-L-alanine) showed the highest GGCT inhibition efficiency. However, since GA had low cell membrane permeability, the diesterified compound, pro-GA, was designed for the purpose of enhancing membrane permeability.
Pro-GA showed a significant inhibition on cell growth in MCF7 breast cancer cell, PC3 prostate cancer cell and HL-60 leukemia cell. Intraperitoneal administration of pro-GA showed a significant tumor growth inhibition in MCF7- and PC3-inoculated mice. Body weight loss and treatment-related death were not observed in these xenograft mice.
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Report
(4 results)
Research Products
(16 results)
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[Journal Article] A novel prodrug of a γ-glutamylcyclotransferase inhibitor suppresses cancer cell proliferation in vitro and inhibits tumor growth in a xenograft mouse model of prostate cancer2018
Author(s)
Ii H, Yoshiya T, Nakata S, Taniguchi K, Hidaka K, Tsuda S, Mochizuki M, Nishiuchi Y, Tsuda Y, Ito K, Kageyama S, Yoshiki T.
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Journal Title
ChemMedChem
Volume: 13
Pages: 155-163
DOI
Related Report
Peer Reviewed / Open Access
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