Development of a new drug for heart failure targeting phospholamban

2015 Fiscal Year Final Research Report

• Project/Area Number: 25293062
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Partial Multi-year Fund
• Section: 一般
• Research Field: General pharmacology
• Research Institution: Yamaguchi University
• Principal Investigator: INUI Makoto 山口大学, 医学(系)研究科(研究院), 教授 (70223237)
• Co-Investigator(Kenkyū-buntansha): KAMIMURA Akio 山口大学, 大学院医学系研究科, 教授 (30194971) ; KURAMASU Atsuo 山口大学, 大学院医学系研究科, 准教授 (90302091) ; HONDA Takeshi 山口大学, 大学院医学系研究科, 講師 (30457311)
• Co-Investigator(Renkei-kenkyūsha): NAMBA Keiichi 大阪大学, 大学院生命機能研究科, 教授 (30346142)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: 心不全治療薬 / ホスホランバン / アプタマー / 創薬

Outline of Final Research Achievements

In the failing heart, the Ca2+ pumping activity of the intracellular Ca2+ storage site, the sarcoplasmic reticulum (SR), is significantly reduced, resulting in dysfunction of cardiomyocytes due to intracellular Ca2+ overload. The Ca2+ pumping activity of SR is regulated by phospholamban, which is a potential target to the treatment of heart failure. Here we studied a phospholamban inhibitor which augments the Ca2+ pumping activity of SR, including a phospholamban aptamer. Our results including optimization of a phospholamban aptamer provide a basis for the development of new therapeutic agents for heart failure.

Free Research Field

薬理学