Macrocyclic Helix‐Threading Peptides for Targeting RNA

Abstract

Ein Ring als Erkennungsmerkmal: RNA bindende makrocyclische Peptide, die durch Helices fädeln, wurden mit einer Ringschlussmetathese an der Festphase erhalten. Die Verbindungen haben eine höhere Affinität zur RNA‐Zielsequenz als ihre linearen Vorstufen, und sie binden auch an eine natürliche mikroRNA‐Vorstufe, sodass sie die mikroRNA‐Funktion steuern könnten.

Triple‐Helical Recognition of RNA Using 2‐Aminopyridine‐Modified PNA at Physiologically Relevant Conditions

“…While this is a relatively new area of research, Beal and co-workers [27] have already demonstrated the potential of targeting pri-miRNAs using helix-threading peptides. For triple-helical RNA recognition, modulation of nucleobase basicity (cf.…”

Triple‐Helical Recognition of RNA Using 2‐Aminopyridine‐Modified PNA at Physiologically Relevant Conditions

“…In preliminary experiments nucleobase-modified PNA recognized a purine rich model sequence of a double helical miRNA precursor with high affinity at physiologically relevant conditions. While this is a relatively new area of research, Beal and co-workers [27] have already demonstrated the potential of targeting pri-miRNAs using helix-threading peptides. Taken together our results suggest that PNA may have unique and previously underappreciated potential for triple helical recognition of biologically relevant RNA.…”

Molecular simulation studies of 3,3′-Diindolylmethane as a Potent MicroRNA-21 Antagonist

“…[ 34 35 36 37 38 ] Furthermore, high affinity synthetic small molecule ligands have been recently described to bind with pre-miRNA. [ 38 39 40 ] In this regard, we aim to analyze the binding properties of 3,3′-diindolylmethane (DIM) with pre-miR-21, as a potential inhibitor of miR-21. DIM is a natural compound that is abundant in cruciferous vegetables such as broccoli, cauliflower, and cabbage, and it is a major acid condensation product of indole-3-carbinol.…”