Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 28, Issue 43, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.202104618
Keywords
biotin; cancer cell targeting; cell-penetrating peptides; gene technology; small molecules
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Funding
- Evonik Industries AG
- DFG
- Projekt DEAL
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This study reported a transfection vector that can home in on tumors by combining biotin, which mediates cell selectivity, with a DNA-binding motif via a hydrophilic linker. It showed a preference for the BR-positive cell lines over the BR-negative controls.
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.
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