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Solution Structure of a G‐quadruplex Bound to the Bisquinolinium Compound Phen‐DC 3
Author(s) -
Chung Wan Jun,
Heddi Brahim,
Hamon Florian,
TeuladeFichou MariePaule,
Phan Anh Tuân
Publication year - 2014
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201308063
Subject(s) - g quadruplex , stacking , chemistry , intramolecular force , tetrad , guanine , stereochemistry , nuclear magnetic resonance spectroscopy , dna , biochemistry , biology , nucleotide , gene , genetics , organic chemistry
Phen‐DC 3 is a highly promising compound that specifically targets G‐quadruplexes, with potent biological effects observed in vivo. We used NMR spectroscopy to solve the structure of the complex formed between Phen‐DC 3 and an intramolecular G‐quadruplex derived from the c‐myc promoter. Structural information revealed that Phen‐DC 3 interacts with the quadruplex through extensive π‐stacking with guanine bases of the top G‐tetrad. On the basis of our structure, modifications are proposed for the development of this compound for selective targeting of a specific G‐quadruplex conformation.