Development of highly constrained nucleic acid analogue based on norbornane structure

• Project/Area Number: 25893305
• Research Category: Grant-in-Aid for Research Activity Start-up
• Allocation Type: Single-year Grants
• Research Field: Chemical pharmacy
• Research Institution: 独立行政法人医薬基盤研究所
• Principal Investigator: MORIHIRO Kunihiko 独立行政法人医薬基盤研究所, 創薬支援スクリーニングセンター, 特任研究員 (70713890)
• Project Period (FY): 2013-08-30 – 2015-03-31
• Project Status: Completed (Fiscal Year 2014)
• Budget Amount: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000); Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000); Fiscal Year 2013: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
• Keywords: 人工核酸 / ノルボルナン / エントロピー / 遺伝子発現制御 / オリゴヌクレオチド

Outline of Final Research Achievements

In this research, I designed and developed nucleic acid analogues for minimizing the loss of entropy with the formation of nucleic acid complexes. I firstly attempted to develop a highly constrained nucleic acid analogue based on a norbornane structure. As a result, I synthesized an important intermediate for the construction of norbornane structure. However, It was difficult to proceed with further derivatization. Therefore, I newly designed a nucleic acid analogue based on oxi-norbornane structure. I successfully introduced a nucleobase and further derivatization is now proceeding.