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{Pont:2020:10.1002/cbic.201900678,
author = {Pont, I and Martínez-Camarena, Á and Galiana-Roselló, C and Tejero, R and Albelda, MT and González-García, J and Vilar, R and García-España, EV},
doi = {10.1002/cbic.201900678},
journal = {ChemBioChem: a European journal of chemical biology},
pages = {1167--1177},
title = {Development of polyamine substituted triphenylamine ligands with high affinity and selectivity for G-quadruplex DNA},
url = {http://dx.doi.org/10.1002/cbic.201900678},
volume = {21},
year = {2020}
}

RIS format (EndNote, RefMan)

TY  - JOUR
AB - Currently significant efforts are devoted to designing small molecules able to bind selectively to guanine-quadruplexes (G4s). These non-canonical DNA structures are implicated in various important biological processes and have been identified as potential targets for drug development. Previously, we reported a series of triphenylamine(TPA)-based compounds including macrocyclic polyamines, which display high affinity towards G4 DNA. Following from this initial work, herein we present a series of second-generation compounds, in which the central TPA has been functionalised with flexible and adaptive linear polyamines, aiming to maximise the selectivity towards G4 DNA. The acid-base properties of the new derivatives have been studied by means of potentiometric titrations, UV-Vis and fluorescence emission spectroscopies. The interaction with G4s and duplex DNA has been explored using FRET melting assays, fluorescence spectroscopy and circular dichroism. Compared to our previously TPA derivatives with macrocyclic substituents, the new ligands reported herein retain the G4 affinity, but display two orders of magnitude higher selectivity for G4 vs. duplex DNA, most likely due to the ability of the linear substituents to embrace the G4 structure.
AU - Pont,I
AU - Martínez-Camarena,Á
AU - Galiana-Roselló,C
AU - Tejero,R
AU - Albelda,MT
AU - González-García,J
AU - Vilar,R
AU - García-España,EV
DO - 10.1002/cbic.201900678
EP - 1177
PY - 2020///
SN - 1439-4227
SP - 1167
TI - Development of polyamine substituted triphenylamine ligands with high affinity and selectivity for G-quadruplex DNA
T2 - ChemBioChem: a European journal of chemical biology
UR - http://dx.doi.org/10.1002/cbic.201900678
UR - https://www.ncbi.nlm.nih.gov/pubmed/31701633
UR - http://hdl.handle.net/10044/1/75639
VL - 21
ER -