Advances towards Cell‐Specific Gene Transfection : A Small‐Molecule Approach Allows Order‐of‐Magnitude Selectivity
In: Chemistry - A European Journal, Vol. 28 (2022), No. 43, p. e202202024
2022article/chapter in journalOA Hybrid
ChemistryBiologyFaculty of Biology » MolekularbiologieFaculty of Chemistry » Organische ChemieScientific institutes » Center of Medical Biotechnology (ZMB)
Related: 1 publication(s)
Title in English:
Advances towards Cell‐Specific Gene Transfection : A Small‐Molecule Approach Allows Order‐of‐Magnitude Selectivity
Author:
Dirksmeyer, Thies;Stahl, Paul
- ORCID
- 0000-0001-6300-0006
- GND
- 130722069X
- LSF ID
- 59461
- ORCID
- 0000-0002-9413-846X
- Other
- connected with university
- LSF ID
- 51606
- ORCID
- 0000-0003-4321-0924
- Other
- connected with university
- GND
- 101888906X
- LSF ID
- 56454
- ORCID
- 0000-0001-6355-536X
- Other
- connected with university
- GND
- 124651291
- LSF ID
- 49829
- ORCID
- 0000-0001-6062-0357
- Other
- connected with university
- LSF ID
- 54494
- ORCID
- 0000-0002-9409-1550
- Other
- connected with university
corresponding author
Year of publication:
2022
Open Access?:
OA Hybrid
Web of Science ID
PubMed ID
Scopus ID
Language of text:
English
Abstract in English:
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.