Advances Towards Cell-Specific Gene Transfection: A Small-Molecule Approach Allows Order-of-Magnitude Selectivity
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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.
Dual activity inhibition of threonine aspartase 1 by a single bisphosphate ligand.
Hoing A, Struth R, Beuck C, Rafieiolhosseini N, Hoffmann D, Stauber R RSC Adv. 2022; 12(53):34176-34184.
PMID: 36545626 PMC: 9709806. DOI: 10.1039/d2ra06019a.
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PMID: 35604769 PMC: 9401007. DOI: 10.1002/chem.202104618.