G-quadruplex-specific peptide-hemicyanine ligands by partial combinatorial selection.
G-quadruplex DNA-specific ligands were generated using a combinatorial selection of tetrapeptides which were then conjugated to a hemicyanine scaffold. 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.
University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK.
James A
JA
Schouten
Sylvain
S
Ladame
Stephen J
SJ
Mason
Matthew A
MA
Cooper
Shankar
S
Balasubramanian
D002232:Carbocyanines / Q000737:chemistry*; D004396:Coloring Agents / Q000737:chemistry; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D004247:DNA / Q000737:chemistry* / Q000378:metabolism; D054856:G-Quadruplexes; D007700:Kinetics; D008024:Ligands; D009842:Oligopeptides / Q000737:chemistry* / Q000378:metabolism; D013379:Substrate Specificity; D020349:Surface Plasmon Resonance
D002232:Carbocyanines; D004396:Coloring Agents; D008024:Ligands; D009842:Oligopeptides; D004247:DNA