title: Stapling monomeric GCN4 peptides allows for DNA binding and enhanced cellular uptake.
abstract: The basic DNA recognition region of the GCN4 protein comprising 23 amino acids has been modified to contain two optimally positioned cysteines which have been linked and stapled using cross-linkers of suitable lengths. This results in stapled peptides with a stabilized α-helical conformation which allows for DNA binding and concurrent enhancement of cellular uptake.
authors.affiliation: Organic and Biomimetic Chemistry Research Group, Krijgslaan 281, S4, B-9000 Gent, Belgium. annemieke.madder@ugent.be.
authors.forename: Abhishek
authors.initials: A
authors.lastname: Iyer
authors.forename: Dorien
authors.initials: D
authors.lastname: Van Lysebetten
authors.forename: Yara
authors.initials: Y
authors.lastname: Ruiz García
authors.forename: Benoit
authors.initials: B
authors.lastname: Louage
authors.forename: Bruno G
authors.initials: BG
authors.lastname: De Geest
authors.forename: Annemieke
authors.initials: A
authors.lastname: Madder
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001483:Base Sequence; D050976:Basic-Leucine Zipper Transcription Factors / Q000737:chemistry*; D004247:DNA / Q000235:genetics / Q000378:metabolism*; D015195:Drug Design; D051379:Mice; D008969:Molecular Sequence Data; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D017433:Protein Structure, Secondary; D021381:Protein Transport; D000067996:RAW 264.7 Cells; D029701:Saccharomyces cerevisiae Proteins / Q000737:chemistry*
chemical_list: D050976:Basic-Leucine Zipper Transcription Factors; C501391:GCN4 protein, S cerevisiae; D010446:Peptide Fragments; D029701:Saccharomyces cerevisiae Proteins; D004247:DNA