Drug discovery research based on dinuclear platinum complexes with markedly high antitumor activity
| Project/Area Number |
15K07905
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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 |
Physical pharmacy
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| Research Institution | Suzuka University of Medical Science |
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Principal Investigator |
Komeda Seiji 鈴鹿医療科学大学, 薬学部, 准教授 (60425056)
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| Co-Investigator(Kenkyū-buntansha) |
植村 雅子 鈴鹿医療科学大学, 薬学部, 助教 (70511997)
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| Co-Investigator(Renkei-kenkyūsha) |
HIRAMOTO Keiichi 鈴鹿医療科学大学, 薬学部, 助教 (90251793)
HARUSAWA Shinya 大阪薬科大学, 薬学部, 教授 (90167601)
YONEYAMA Hiroki 大阪薬科大学, 薬学部, 助教 (90627001)
YOSHIKAWA Yuko 同志社大学, 生命医科学部, 嘱託講師 (80291871)
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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 |
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2017: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | 白金錯体 / 制がん剤 / DDS / 創薬 / 難治性がん / 白金製剤 / オキサリプラチン / 大腸がん / 抗腫瘍効果 / 細胞内蓄積 / 白金制がん剤 / 金属錯体 / 核酸 / 細胞内取込 / 薬物耐性 |
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| Outline of Final Research Achievements |
New tetrazolato-bridged dinuclear platinum(II) complexes were designed and synthesized to combine with DDS carrier or to introduce halogen into the complexes. Our in vivo study using mice with a subcutaneous homograft of Colon-26 colorectal cancer cells indicates that the tetrazolato-bridged dinuclear platinum(II) complexes are promising next-generation platinum-based drug candidates with markedly high and long-lasting antitumor efficacy. Indeed, the tumour growth in mice treated with the lead compound was much slower than that in mice treated with platinum-based drug oxaliplatin, which is used for the treatment of colorectal cancer. Even more remarkable, the lead compound exhibited high tumor-reduction effects against large-sized tumours, which sustained for a few weeks after a single intravenous dose of the compound.
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Report
(4 results)
Research Products
(27 results)
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[Journal Article] Chromatin folding and DNA replication inhibition mediated by a highly antitumor-active tetrazolato-bridged dinuclear platinum(II) complex.2016
Author(s)
Imai R, Komeda S, Shimura M, Tamura S, Matsuyama S, Nishimura K, Rogge R, Matsunaga A, Hiratani I, Takata H, Uemura M, Iida Y, Yoshikawa Y, Hansen JC, Yamauchi K, Kanemaki MT, Maeshima K.
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Journal Title
Scientific Reports
Volume: 6
Issue: 1
Pages: 24712-24725
DOI
Related Report
Peer Reviewed / Open Access / Int'l Joint Research
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[Presentation] 制がん白金(II)二核錯体のDNA凝縮能および細胞内取り込みに関する研究2017
Author(s)
植村雅子, 米山弘樹, 岡本直人, 村松 晃, 福田青郎, 小西宏明, 髙木 陽光, 松﨑 健, 春沢信哉, 吉川祐子, 今中忠行, 吉川研一，米田誠治
Organizer
第63回日本薬学会東海支部 総会・大会
Related Report
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[Presentation] 長短鎖アルキル基を導入した制がんテトラゾラト架橋白金(II)二核錯体の細胞 内取込およびDNA凝縮能2016
Author(s)
米田誠治, 植村雅子, 米山弘樹, 岡本直人, 村松 晃, 福田青郎, 小西宏明, 髙木 陽光, 松﨑 健, 春沢信哉, 吉川祐子, 今中忠行, 吉川研一
Organizer
日本薬学会 第136年会 横浜市 年月日201603-201603
Place of Presentation
横浜市
Year and Date
2016-03-26
Related Report
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[Presentation] Action of novel anticancer-active, dinuclear platinum complexes with ester group on the higher order structure and genomic activity of DNA2015
Author(s)
Shimizu, Y; Yoshikawa, Y; TaTsuchiya, T; Hiroki Yoneyama, H; Harusawa, S; Komeda, S; Imanaka, T; Kenmotsu, T; Yoshikawa, K.
Organizer
第53回生物物理学会日本薬学会
Place of Presentation
金沢市
Year and Date
2015-09-13
Related Report
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