2013 Fiscal Year Final Research Report
Design and Synthesis of the Artificial Luminescent Death Ligands Based on C3-Symmetric Cyclometalated Iridium Complexes for Selective Staining and Apoptosis Induction of Cancer Cells
| Project/Area Number |
24890256
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| Research Category |
Grant-in-Aid for Research Activity Start-up
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| Allocation Type | Single-year Grants |
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| Research Field |
Chemical pharmacy
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| Research Institution | Tokyo University of Science |
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Principal Investigator |
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| Project Period (FY) |
2012-08-31 – 2014-03-31
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| Keywords | がん治療薬 / イリジウム錯体 / 燐光 / ペプチド / pHプローブ |
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| Research Abstract |
TNF-related apoptosis-inducing ligand (TRAIL) having a C3-symmetric homotrimeric structure induces the apoptosis in various tumor cells and tissues through the interaction with death receptor (DR) on cell surface. In this study, we have addressed the design and synthesis of new C3-symmetric tris-cyclometalated Ir complexes having dual activity both agonist activity for apoptosis induction and luminescent imaging of cancer cells.Staining experiments of Jurkat cell with Ir complex having the DR5 binding cyclic peptide suggested that green emission was localized on the cell membrane. Moreover, flow cytometer analysis suggested that the correlation between DR5 expressions of cancer cells (Jurkat cells, Molt-4 cells, K562 cells) and emission intensities derived from Ir complex. Optimizations of Ir complexes for improvement of their TRAIL-like activity are undergoing.
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Research Products
(29 results)
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[Presentation] Design, Synthesis and Biological Applications of Luminescent Cyclometalated Ir(III) Complexes2013
Author(s)
Yosuke Hisamatsu, Aya Kando, Shinsuke Moromizato, Ai Shibuya, Hiroshi Tanaka, Akihiro Nakagawa, Toshihiro Suzuki, Ryo Abe and Shin Aoki, 鈴木利宙,安部良,青木伸
Organizer
第57回日本薬学会関東支部大会
Place of Presentation
東京
Year and Date
20131000
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