Imperial College London

Prof. Ramon Vilar

Faculty of Natural SciencesDepartment of Chemistry

Professor of Medicinal Inorganic Chemistry
 
 
 
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Contact

 

+44 (0)20 7594 1967r.vilar Website

 
 
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Location

 

301HMolecular Sciences Research HubWhite City Campus

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Summary

 

Publications

Citation

BibTex format

@article{Vilar:2019:10.1002/chem.201901569,
author = {Vilar, R and Ruehl, CL and Lim, AHM and Kench, T and Mann, DJ},
doi = {10.1002/chem.201901569},
journal = {Chemistry - A European Journal},
pages = {9691--9700},
title = {An octahedral cobalt(III) complex with axial NH3 ligands that templates and selectively stabilises G-quadruplex DNA},
url = {http://dx.doi.org/10.1002/chem.201901569},
volume = {25},
year = {2019}
}

RIS format (EndNote, RefMan)

TY  - JOUR
AB - Guanine-rich sequences of DNA are known to readily fold into tetra-stranded helical structures known as G-quadruplexes (G4). Due to their biological relevance, G4s are potential anticancer drug targets and therefore there is significant interest in molecules with high affinity for these structures. Most G4 binders are polyaromatic planar compounds which π-π stack on the G4's guanine tetrad. However, many of these compounds are not very selective since they can also intercalate into duplex DNA. Herein we report a new class of binder based on an octahedral cobalt(III) complex that binds to G4 via a different mode involving hydrogen-bonding, electrostatic interactions and π-π stacking. We show that this new compound binds selectivity to G4 over duplex DNA (particularly to the G-rich sequence of the c-myc promoter). This new octahedral complex also has the ability to template he formation of G4 DNA from the unfolded sequence. Finally, we show that upon binding to G4, the complex prevents helicase Pif1-p from unfolding the c-myc G4 structure.
AU - Vilar,R
AU - Ruehl,CL
AU - Lim,AHM
AU - Kench,T
AU - Mann,DJ
DO - 10.1002/chem.201901569
EP - 9700
PY - 2019///
SN - 0947-6539
SP - 9691
TI - An octahedral cobalt(III) complex with axial NH3 ligands that templates and selectively stabilises G-quadruplex DNA
T2 - Chemistry - A European Journal
UR - http://dx.doi.org/10.1002/chem.201901569
UR - https://www.ncbi.nlm.nih.gov/pubmed/31087710
UR - https://onlinelibrary.wiley.com/doi/full/10.1002/chem.201901569
UR - http://hdl.handle.net/10044/1/70511
VL - 25
ER -