Conformationally restricted polyamines: Solid-phase synthesis and biological evaluation

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K08027
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Nagoya City University
• Principal Investigator: Umezawa Naoki 名古屋市立大学, 大学院薬学研究科, 准教授 (40347422)
• Co-Investigator(Renkei-kenkyūsha): YOSHIKAWA Kenichi 同志社大学, 生命医科学部, 教授 (80110823) ; YOSHIKAWA Yuko 立命館大学, 生命科学部, 教授 (80291871) ; UMEHARA Takashi 独立行政法人理化学研究所, 生命機能科学研究センター・エピジェネティクス制御研究ユニット, ユニットリーダー (20415095) ; INOUE Katsuhisa 東京薬科大学, 薬学部, 教授 (50315892)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: ポリアミン / 固相合成

Outline of Final Research Achievements

Polyamines are organic cations containing multiple amino groups, and are found in all living organisms. In most cases, polyamines have flexible structure and show wide variety of biological functions. We have been developing solid-phase synthesis of polyamines based on peptide chemistry; the peptide on the solid support was exhaustively reduced and crude polyamine thus obtained was purified by reversed-phase HPLC.
In this research, we have improved our solid-phase synthesis for branched and cyclic polyamines. Also, we have evaluated following 4 functions of synthesized polyamines, 1) the effect on DNA duplex structure, 2) lysine-specific demethylases inhibition, 3) prevention of thermal inactivation of protein, and 4) effect on ribozyme activity.

Free Research Field

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