We gratefully acknowledge D. Grierson for fruitful discussion, Marianne Blombled for LC-MS analysis, the MENRT for a PhD fellowship to M.R.D., the CNRS and the Institut Curie for a joint PhD fellowship to E.L., the LNCC for a grant (Equipe Labellisée) to J.F.R. and a PhD fellowship to A.S., and the ANR for financial support to F.H. (ANR-09-BLAN-0355 “G4Toolbox”). Nicolas Saettel is especially acknowledged for his help in the docking experiment.
An Acyclic Oligoheteroaryle That Discriminates Strongly between Diverse G-Quadruplex Topologies†
Article first published online: 2 AUG 2011
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 50, Issue 37, pages 8745–8749, September 5, 2011
How to Cite
Hamon, F., Largy, E., Guédin-Beaurepaire, A., Rouchon-Dagois, M., Sidibe, A., Monchaud, D., Mergny, J.-L., Riou, J.-F., Nguyen, C.-H. and Teulade-Fichou, M.-P. (2011), An Acyclic Oligoheteroaryle That Discriminates Strongly between Diverse G-Quadruplex Topologies. Angew. Chem. Int. Ed., 50: 8745–8749. doi: 10.1002/anie.201103422
- Issue published online: 1 SEP 2011
- Article first published online: 2 AUG 2011
- Manuscript Received: 18 MAY 2011
- ANR. Grant Number: ANR-09-BLAN-0355
- molecular recognition
Feeling groovy: A family of nonmacrocyclic G-quadruplex binders with alternate oxazole and pyridine motifs was prepared. The shown heptacyclic derivative exhibits an unprecedented binding preference for certain quadruplex topologies: it recognizes exclusively the human telomeric quadruplex in Na+ buffer but not in K+ buffer. This unique quadruplex binding profile is strongly dependent on the size of the ligand and may result from groove interactions.