期刊
CHEMICAL COMMUNICATIONS
卷 56, 期 85, 页码 12905-12908出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0cc04957c
关键词
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资金
- Japan Society for the Promotion of Science (JSPS) [20H02876, 19K05743, 20K15411, 18H04387, 20H04789]
- Japan Science and Technology Agency (JST) [ACT-X JPMJAX191E]
- Nippon Foundation
- Inamori Grants
- Translational Research program
- Strategic PRomotion for practical application of INnovative medical Technology (TR-SPRINT) from the Japan Agency for Medical Research and Development
- KAKENHI [16H06276]
- National Research Foundation of Korea [4120200213576] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
- Grants-in-Aid for Scientific Research [18H04387, 20H02876, 20H04789, 20K15411, 19K05743] Funding Source: KAKEN
Macrocyclic hexaoxazoles (6OTDs) are G-quadruplex (G4) ligands, and some derivatives, such as L2H2-6OTD (1a) bearing two aminobutyl side chains, show cytotoxicity towards cancer cells. To identify the cellular target of 1a, we employed a post-target-binding strategy utilizing click reaction (Huisgen cyclization) between the azide-conjugated ligand L2H2-6OTD-Az (1b) and the cell-permeable dye CO-1 bearing a strained alkyne moiety and the BODIPY fluorophore under Cu-free conditions. We confirmed that introduction of the small azide group did not alter the physical or biological properties, including anti-cancer activity, of 1a, and we also demonstrated bias-free localization of CO-1. The post-binding visualization strategy suggested that L2H2-6OTD (1a) colocalized with RNA G4 in living cells.
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