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Utilizing Combinatorial Chemistry and Rational Design: Peptidic Tweezers with Nanomolar Affinity to DNA Can Be Transformed into Efficient Vectors for Gene Delivery by Addition of a Lipophilic Tail
Author(s) -
Kuchelmeister Hannes Y.,
Karczewski Sarah,
Gutschmidt Aljona,
Knauer Shirley,
Schmuck Carsten
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201306929
Subject(s) - tweezers , gene delivery , dna , transfection , rational design , combinatorial chemistry , computational biology , chemistry , peptide , gene , optical tweezers , computer science , biochemistry , nanotechnology , biology , materials science , physics , quantum mechanics
Into the library: Screening a focused library of 259 peptide tweezers, composed of two identical arms with zero to three amino acids and an artificial anion recognition site, yielded DNA binders with nanomolar affinity. These ligands are only modest gene carriers (transfection efficiency <10 %); however, excellent transfection efficiencies (up to 90 %) were achieved after the covalent attachment of long aliphatic chains.