From alkylating to shape-shifting G-quadruplex ligands: the RHAU peptide story.

ABSTRACT: G-quadruplexes (G4s) are non-canonical secondary nucleic acid structures with important biological implications in telomere elongation and gene expression. A large number of small molecules have been developed to bind and even covalently target these structures, enhancing the potency and duration of binding. Alternatively, peptide-based ligands have been studied and shown to offer several advantages, including high specificity, a modular design, and ease of synthesis. In this work, we describe a peptide-based methodology for covalent G4-targeting, based on the introduction of two photoactivatable moieties in a peptide derived from the RHAU helicase. Rational insertion of crosslinkers at different positions yielded nine different peptides, which were evaluated for their G4-stabilizing effec

SUBMITTER: De Paepe L 

PROVIDER: S-EPMC12852953 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature