Development of phospholamban aptamer as a treatment of heart failure for clinical application

2016 Fiscal Year Final Research Report

• Project/Area Number: 15K18989
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: General pharmacology
• Research Institution: Yamaguchi University
• Principal Investigator: SAKAI Hiroki 山口大学, 医学(系)研究科(研究院), 助教 (40464367)
• Project Period (FY): 2015-04-01 – 2017-03-31
• Keywords: 心不全治療薬 / アプタマー / 細胞膜透過性ペプチド / ホスホランバン

Outline of Final Research Achievements

We tried to develop a cell-penetrating phospholamban aptamer as a novel therapeutic tool for treatment of heart failure. We optimized the nucleotide sequence of the phospholamban aptamer which retains the functional activity and is stable in the serum. The obtained phospholamban aptamer enhanced contraction/relaxation of isolated adult rat cardiomyocytes as well as corresponding Ca2+ transients. However, no consistent improvement of cardiac function was obtained in a mouse heart failure model by administration of the aptamer. Further modification would be necessary to improve the pharmacokinetic property of the aptamer for clinical application.

Free Research Field

薬理学