Development of highly-sensitive apoptosis imaging agent based on new drug design

Research Project

Project/Area Number	26461785
Research Category	Grant-in-Aid for Scientific Research (C)
Allocation Type	Multi-year Fund
Section	一般
Research Field	Radiation science
Research Institution	Gunma University
Principal Investigator	Hanaoka Hirofumi 群馬大学, 大学院医学系研究科, 特任准教授 (50361390)
Co-Investigator(Kenkyū-buntansha)	上原知也千葉大学, 大学院薬学研究院, 准教授 (10323403)
Project Period (FY)	2014-04-01 – 2017-03-31
Project Status	Completed (Fiscal Year 2016)
Budget Amount *help	¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000) Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000) Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000) Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Keywords	放射性医薬品 / アポトーシス / 放射性医薬品・造影剤
Outline of Final Research Achievements	The aim of this study was to develop highly-sensitive apoptosis imaging agent for early prediction of anti-cancer therapy. One of the early biochemical changes of apoptotic cells is exposure of phosphatidylserine (PS) on the external surface of the plasma membrane. The LIKKPF, with high affinity for PS, was selected as a mother compound, then D-amino acid peptide fpkkil-NH2 was designed and prepared considering stability. The fpkkil-NH2 maintained affinity to PS and was stable in vivo. Thus, radiolabeled fpkkil-NH2 derivatives will be useful as apoptosis imaging agents.