title: Cyclodextrin-peptide conjugates for sequence specific DNA binding.
abstract: Synthetic models of bZIP transcription factors have been developed with the capability of specific DNA recognition. Our design is based on the CuAAC mediated conjugation of basic region Leucine Zipper peptides to different derivatives of α, β and γ-cyclodextrins equipped with azide functionalities. Thorough optimization of reaction conditions allowed convergent and simultaneous conjugation of two long unprotected cationic peptides to cyclodextrin-bis azide derivatives. The resulting constructs were shown to specifically recognize their cognate DNA sequence with nM affinities. In comparison with previously developed TF models, the derivatives described here combine the enhanced DNA binding capabilities with an easy and convergent synthetic route.
authors: Organic and Biomimetic Chemistry Research Group, Department of Organic and Macromolecular Chemistry, Ghent University, Krijgslaan 281 (S4), B-9000 Ghent, Belgium. annemieke.madder@ugent.be.
authors: Yara
authors: Y
authors: Ruiz García
authors: Jan
authors: J
authors: Zelenka
authors: Y Vladimir
authors: YV
authors: Pabon
authors: Abhishek
authors: A
authors: Iyer
authors: Miloš
authors: M
authors: Buděšínský
authors: Tomáš
authors: T
authors: Kraus
authors: C I Edvard
authors: CI
authors: Smith
authors: Annemieke
authors: A
authors: Madder
mesh_terms: D003505:Cyclodextrins / Q000737:chemistry*; D004247:DNA / Q000737:chemistry*; D010455:Peptides / Q000737:chemistry*
chemical_list: D003505:Cyclodextrins; D010455:Peptides; D004247:DNA