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Nucleic Acids Symposium Series 2008 52(1):165-166; doi:10.1093/nass/nrn084
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© 2008 Oxford University Press

This article appears in the following Nucleic Acid Symposium Series issue: Joint Symposium of the 18th International Roundtable on Nucleosides, Nucleotides and Nucleic Acids and the 35th International Symposium on Nucleic Acids Chemistry [View the issue table of contents]

Ligand binding to tetra-end-linked (TGGGGT)4 G-quadruplexes: an electrospray mass spectroscopy study

Jussara Amato1, Giorgia Oliviero1, Nicola Borbone1, Stefano D’Errico1, Gennaro Piccialli1, Patrick Mailliet2, Frédéric Rosu3, Edwin De Pauw3 and Valérie Gabelica*,3

1Dipartimento di Chimica delle Sostanze Naturali, Università degli Studi di Napoli "Federico II", Via D. Montesano 49, I-80131 Napoli, Italy. 2Sanofi-Aventis, Centre de Recherches de Paris, Vitry-sur-Seine, France and 3Laboratoire de Spectrométrie de Masse, Université de Liège, Institut de Chimie Bat. B6c, B-4000 Liège, Belgium

*Corresponding Author. E-mail: v.gabelica{at}ulg.ac.be

Abstract

The binding properties of a series of known G-quadruplex ligands have been studied by ESI-MS experiments. The tetramolecular (TG4T)4 quadruplex and its analogues I and II blocked, respectively, at the 3' or 5'-end by a tetra-end-linker (TEL) unit were chosen as the ligands targets. The stoichiometries of the obtained complexes as well as the ligand affinity and selectivity to the different quadruplexes were determined to deduce the ligand binding site. The TEL derivatives I and II allowed the probing of the grooves contribution to the binding of ligands to G-quadruplexes, demonstrating that the 3' and 5' quartets are not equivalent binding sites for ligand end-stacking.


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