Comparison of library screening techniques used in the development of dsDNA ligands.
The gel retardation and FID (fluorescent intercalator displacement) techniques have been compared for the selection of dsDNA binding ligands out of library mixtures. The selection procedure involves the synthesis and screening of unnatural oligopeptide libraries based on an iterative deconvolution procedure. Both methods yield comparable selection results and binding constants for the selected compounds, meaning that they can be considered as complementary in the discovery process of new antigene compounds. Furthermore, a quinazolin-2,4-dione amino acid has been identified as possessing interesting properties for interaction with dsDNA.
Chaltin
Patrick
P
Laboratory of Medicinal Chemistry, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, Belgium.
Borgions
Filip
F
Van Aerschot
Arthur
A
Herdewijn
Piet
P
D000596:Amino Acids / Q000737:chemistry; D004247:DNA / Q000378:metabolism*; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D024202:Electrophoretic Mobility Shift Assay; D005456:Fluorescent Dyes; D008024:Ligands; D009842:Oligopeptides / Q000138:chemical synthesis / Q000378:metabolism; D019151:Peptide Library
D000596:Amino Acids; D005456:Fluorescent Dyes; D008024:Ligands; D009842:Oligopeptides; D019151:Peptide Library; D004247:DNA