Design and synthesis of new cationic metal complexes for anticancer drugs and identification of their target molecules

2017 Fiscal Year Final Research Report

• Project/Area Number: 16K18851
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Chemical pharmacy
• Research Institution: Nagoya City University
• Principal Investigator: Hisamatsu Yosuke 名古屋市立大学, 大学院薬学研究科, 講師 (80587270)
• Project Period (FY): 2016-04-01 – 2018-03-31
• Keywords: がん治療薬 / イリジウム錯体 / カチオン性ペプチド / 細胞死 / ペプチド

Outline of Final Research Achievements

In this work, we have continued the mechanistic studies of cell death induced by amphiphilic Ir complexes containing cationic peptides. We designed and synthesized new cationic amphiphilic Ir complexes having photoreactive diazirine groups for photoaffinity labeling to identify the target molecules of the Ir complex. A proteomic analysis of the products obtained by the photoirradiation of Ir complex with Jurkat cells suggests that the Ca2+-binding protein “calmodulin (CaM)” is one of target proteins of the Ir complexes. Indeed, cationic amphiphilic Ir complex forms a stable complex with the Ca2+-CaM complex, as evidenced by luminescence titration experiments.

Free Research Field

生物有機化学、錯体化学