Development of high-throughput screening methods for antisense oligonucleotides

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K17886
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Bio-related chemistry
• Research Institution: Tokyo University of Science
• Principal Investigator: Hara Rintaro 東京理科大学, 薬学部生命創薬科学科, 助教 (70709766)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: アンチセンス核酸医薬 / リボヌクレアーゼH（RNase H） / スクリーニング / カチオン性オリゴ糖 / カチオン性オリゴペプチド

Outline of Final Research Achievements

Antisense oligonucleotides (ASOs) are a promising candidate for nucleic acid drugs. In this study, we aimed to develop high-throughput screening methods in which high-active ASOs are chemically marked. Although we found some functional groups which have appropriate reactivity for these methods, we could not establish the efficient high-throughput screening method. On the other hand, I unintendedly found that some artificial cationic molecules could inhibit the cleavage reaction of mismatched RNAs by ASO and RNase H, which lead directly to side-effects of ASO-type drugs.

Free Research Field

生体関連化学