Dynamic combinatorial chemistry: on the road to fulfilling the promiseSylvain Ladame
Institut de Science et d Ingenierie Supramoleculaires, Universite Louis Pasteur, CNRS UMR 7006, 8, allee Gaspard Monge, BP 70028, 67083 Strasbourg Cedex, France
Org Biomol Chem 6:219-26. 2008
..We present here the most recent advances in the field of dynamic combinatorial chemistry that have been developed to overcome these limitations and explore new areas of application...
Solid-phase synthesis of symmetrical 3,6-bispeptide-acridone conjugatesSylvain Ladame
University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
Org Lett 4:2509-12. 2002
..This strategy will enable the generation of a library of 3,6-bispeptide-acridones to be screened for selective binding to telomeric G-quadruplex DNA...
Templated ligand assembly by using G-quadruplex DNA and dynamic covalent chemistryAndrew M Whitney
University Chemical Laboratories, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
Angew Chem Int Ed Engl 43:1143-6. 2004
Putative DNA quadruplex formation within the human c-kit oncogeneSarah Rankin
Cancer Research UK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, UK
J Am Chem Soc 127:10584-9. 2005
..The c-kit quadruplex may be a new target for therapeutic intervention in cancers where there is elevated expression of the c-kit gene...
Synthesis and spectroscopic and DNA-binding properties of fluorogenic acridine-containing cyanine dyesTariq Mahmood
ISIS Universite de Strasbourg 8, BP 70028, 67083 Strasbourg, France
J Org Chem 75:204-7. 2010
..The mono-, tri-, and pentamethine dyes in particular exhibit promising fluorogenic properties. Their ability to aggregate in solution and to interact with B-DNA is also discussed...
Combining G-quadruplex targeting motifs on a single peptide nucleic acid scaffold: a hybrid (3+1) PNA-DNA bimolecular quadruplexAlexis Paul
Institut de Science et d Ingénierie, Supramoléculaires ISIS, Universite Louis Pasteur, CNRS UMR 7006, 8 allee Gaspard Monge, Strasbourg Cedex, France
Chemistry 14:8682-9. 2008
..These studies could open up new possibilities for the design of a novel generation of quadruplex ligands that target not only the external features of the quadruplex but also its central core constituted by the tetrads themselves...
Discovery of G-quadruplex stabilizing ligands through direct ELISA of a one-bead-one-compound libraryJames E Redman
University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK
Org Biomol Chem 4:4364-9. 2006
..Quadruplex affinity as judged by these surface based techniques was a useful predictor of the ability of the ligands to stabilize the quadruplex to thermal unfolding in solution...
G-quadruplex-specific peptide-hemicyanine ligands by partial combinatorial selectionJames A Schouten
University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
J Am Chem Soc 125:5594-5. 2003
..The heterocycle enhanced peptide binding affinity by approximately 1000-fold to give ligands with near micromolar affinity and >40-fold discrimination for quadruplex DNA over duplex...
Macrocyclic and helical oligoamides as a new class of G-quadruplex ligandsPravin S Shirude
University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
J Am Chem Soc 129:11890-1. 2007
Tetrapeptides induce selective recognition for G-quadruplexes when conjugated to a DNA-binding platformSylvain Ladame
University Chemical Laboratory, University of Cambridge, UK
Org Biomol Chem 2:2925-31. 2004
..These studies indicate that targeting distinct features of a G-quadruplex with hybrid molecules is a promising strategy for discriminating between quadruplex and duplex DNA...
Oxazole-based peptide macrocycles: a new class of G-quadruplex binding ligandsKatja Jantos
The University Chemical Laboratory, University of Cambridge, UK
J Am Chem Soc 128:13662-3. 2006
..Here we provide the first example of a ligand binding to and stabilizing the c-kit quadruplex. Moreover, we show that these macrocycles show a preference for the c-kit quadruplex as compared to the human telomeric quadruplex...
Investigating a quadruplex-ligand interaction by unfolding kineticsJeremy J Green
Department of Chemistry, University of Cambridge, UK
J Am Chem Soc 128:9809-12. 2006
..These results indicate that the presence of the ligand has only a small effect on the activation energy, suggesting that the unbinding of the ligand occurs after the transition state for quadruplex unfolding...
Inhibition of human telomerase activity by an engineered zinc finger protein that binds G-quadruplexesSachin D Patel
Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, United Kingdom
Biochemistry 43:13452-8. 2004
..3 +/- 11.1 nM. Possible molecular mechanisms of inhibition are discussed, together with the potential for using engineered zinc fingers to interfere with the cellular processes associated with telomere function...
Exploring the recognition of quadruplex DNA by an engineered Cys2-His2 zinc finger proteinSylvain Ladame
University Chemical Laboratories, University of Cambridge, UK
Biochemistry 45:1393-9. 2006
..Modeling also suggests that an important role of the key protein finger residues in the Gq1-quadruplex complex is to maintain Gq1 in an optimum conformation for quadruplex recognition...
Targeting nucleic acid secondary structures with polyamides using an optimized dynamic combinatorial approachSylvain Ladame
University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
Angew Chem Int Ed Engl 44:5736-9. 2005
A conserved quadruplex motif located in a transcription activation site of the human c-kit oncogeneHimesh Fernando
Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, United Kingdom
Biochemistry 45:7854-60. 2006
..Collectively, the evidence suggests that this quadruplex is a serious target for a detailed functional investigation at the cell-biology level...