Target identification of a macrocyclic hexaoxazole G-quadruplex ligand using post-target-binding visualization
SCIE
SCOPUS
- Title
- Target identification of a macrocyclic hexaoxazole G-quadruplex ligand using post-target-binding visualization
- Authors
- Yasuda, Mizuho; Ma, Yue; Okabe, Sachiko; Wakabayashi, Yuki; Su, Dongdong; Chang, Young-Tae; Seimiya, Hiroyuki; Tera, Masayuki; Nagasawa, Kazuo
- Date Issued
- 2020-11
- Publisher
- ROYAL SOC CHEMISTRY
- Abstract
- 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.
- URI
- https://oasis.postech.ac.kr/handle/2014.oak/105422
- DOI
- 10.1039/d0cc04957c
- ISSN
- 1359-7345
- Article Type
- Article
- Citation
- CHEMICAL COMMUNICATIONS, vol. 56, no. 85, page. 12905 - 12908, 2020-11
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- There are no files associated with this item.
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