Synthesis of HDAC inhibitors that locally develop their inhibition activity in cells

2014 Fiscal Year Final Research Report

• Project/Area Number: 24659050
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Drug development chemistry
• Research Institution: Nagoya City University
• Principal Investigator: MIYATA Naoki 名古屋市立大学, 薬学研究科(研究院), 教授 (50114674)
• Co-Investigator(Renkei-kenkyūsha): NAKAGAWA Hidehiko 名古屋市立大学, 大学院薬学研究科, 教授 (80281674)
• Research Collaborator: YAMADA Souta
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: ヒストン脱アセチル化酵素 / エピジェネティクス / ケミカルバイオロジー / 細胞内局在性 / 光解除性保護基 / 分子標的治療薬 / 制がん剤 / 蛍光検出

Outline of Final Research Achievements

To elucidate the association between the localization and the function of histone deacetylases (HDACs) in cells, we designed and synthesized HDAC inhibitors which locally develop their activity in cells. We used a caged technique to control the HDAC activity. The synthesized HDAC inhibitors with photo-labile protecting group time-dependently inhibited HDAC activity under the visible light irradiation conditions. These results showed that these HDAC inhibitors can be controlled their activity by visible light irradiation even in the living cell systems and become a useful tool to elucidate the association between the localization and the function of HDAC in cells.

Free Research Field

薬学