Molecular engineering of G-quadruplex ligands based on solvent effect of polyethylene glycol

Because various non-parallel G-quadruplexes of human telomeric sequences in K+ solution can be converted to a parallel G-quadruplex by adding polyethylene glycol (PEG) as a co-solvent, we have taken advantage of this property of PEG to study the covalent attachment of a PEG unit to a G-quadruplex li...

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Bibliographic Details
Published in:Nucleic acids research 2012-09, Vol.40 (17), p.8711-8720
Main Authors: Wang, Zi-Fu, Chang, Ta-Chau
Format: Article
Language:English
Subjects:
Carbazoles - chemistry
Circular Dichroism
G-Quadruplexes
Ligands
Nucleic Acid Denaturation
Polyethylene Glycols - chemistry
Pyridinium Compounds - chemistry
Solvents - chemistry
Structural Biology
Telomere - chemistry
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Summary:Because various non-parallel G-quadruplexes of human telomeric sequences in K+ solution can be converted to a parallel G-quadruplex by adding polyethylene glycol (PEG) as a co-solvent, we have taken advantage of this property of PEG to study the covalent attachment of a PEG unit to a G-quadruplex ligand, 3,6-bis(1-methyl-4-vinylpyridinium) carbazole diiodide (BMVC). The hybrid ligand with the PEG unit, BMVC-8C3O or BMVC-6C2O by substituting either the tetraethylene glycol or the triethylene glycol terminated with a methyl-piperidinium cation in N-9 position of BMVC, not only induces structural change from different non-parallel G-quadruplexes to a parallel G-quadruplex but also increases the melting temperature of human telomeres in K+ solution by more than 45°C. In addition, our ligand work provides further confidence that the local water structure plays the key to induce conformational change of human telomere.
ISSN:0305-1048
1362-4962
DOI:10.1093/nar/gks578