Study on radiolabeling using nucleic acid RNAi medicine

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K15460
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Radiation science
• Research Institution: Gihu University of Medical Science
• Principal Investigator: Nagai Makoto 岐阜医療科学大学, 保健科学部, 准教授 (30460497)
• Co-Investigator(Kenkyū-buntansha): 片渕 哲朗 岐阜医療科学大学, 保健科学部, 教授 (00393231)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: 放射性医薬品 / 核酸医薬品

Outline of Final Research Achievements

Radiopharmaceuticals of RNA medicine have not been found. In this research, we aimed to prepare radioactive nucleic acid drugs that withstand metallic labels and bound to target genes. Molecular design of RNAi drugs that specifically accumulate in human cancer cells even after radiolabeling was designed by molecular orbital method. As a result, substitution at the 5-position hydrogen atom of uracil resulted in not impairing the hybrid ability of the base even when labeling was carried out. Synthetic addition of nonradioactive iodine from BNA or LNA as a raw material was prepared, added to human leukemia cultured cells, and cell growth rate after culturing was measured. The transcription inhibition rate of the synthesized and added RNAi medicine was a result which was not different from usual.

Free Research Field

放射性医薬品

Academic Significance and Societal Importance of the Research Achievements

本研究が目指す成果は、点在するがん細胞等の検査や治療薬として使用できる核酸医薬品の開発である。本研究成果は分子量の大きい放射性物質を核酸断片に結合させることで、核酸断片が金属との凝集の防止と自由度の確保をする分子設計法および分子モデルとして結果が得られた。
放射性物質を用いた核酸分子設計に関する合成法の報告は数少なく学術的にも意義があった。また、今後、細胞内への導入確認および検査・治療等への応用ができれば、点在するがん治療への対応が可能となり社会的意義はあると思われる。