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Chang, Young Tae
복잡계 자기조립 연구단
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Target identification of a macrocyclic hexaoxazole G-quadruplex ligand using post-target-binding visualization

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Title
Target identification of a macrocyclic hexaoxazole G-quadruplex ligand using post-target-binding visualization
Author(s)
Yasuda, M.; Ma, Y.; Okabe, S.; Wakabayashi, Y.; Su, D.; Young-Tae Chang; Seimiya, H.; Tera, M.; Nagasawa, K.
Subject
TELOMERIC G-QUADRUPLEX, ; RNA G-QUADRUPLEXES, ; INHIBITION, ; EXPRESSION, ; BIOLOGY, ; GROWTH, ; END
Publication Date
2020-11
Journal
CHEMICAL COMMUNICATIONS, v.56, no.85, pp.12905 - 12908
Publisher
ROYAL SOC CHEMISTRY
Abstract
© The Royal Society of Chemistry. 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. This journal i
URI
https://pr.ibs.re.kr/handle/8788114/7557
DOI
10.1039/d0cc04957c
ISSN
1359-7345
Appears in Collections:
Center for Self-assembly and Complexity(복잡계 자기조립 연구단) > 1. Journal Papers (저널논문)
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