| Institution: | 1. Institute of Organic Chemistry, University of Duisburg-Essen, 45117 Essen, Germany
These authors contributed equally to this work.;2. Institute of Biology, University of Duisburg-Essen, 45117 Essen, Germany;3. Institute of Organic Chemistry, University of Duisburg-Essen, 45117 Essen, Germany |
| Abstract: | A transfection vector that can home in on tumors is reported. Whereas previous vectors that allow moderately cell selective gene transfection used larger systems, this small-molecule approach paved the way for precise structure-activity relationship optimization. For this, biotin, which mediates cell selectivity, was combined with the potent DNA-binding motif tetralysine-guanidinocarbonypyrrol via a hydrophilic linker, thus enabling SAR-based optimization. The new vector mediated biotin receptor (BR)-selective transfection of cell lines with different BR expression levels. Computer-based analyses of microscopy images revealed a preference of one order of magnitude for the BR-positive cell lines over the BR-negative controls. |
