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Related Experiment Video

Updated: May 16, 2026

Aptamer-Based Target Detection Facilitated by a 3-Stage G-Quadruplex Isothermal Exponential Amplification Reaction
03:38

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Targeting loop adenines in G-quadruplex by a selective oxirane.

Filippo Doria1, Matteo Nadai2, Marco Folini3

  • 1Dipartimento di Chimica, Università di Pavia, V.le Taramelli 10, 27100 Pavia (Italy).

Chemistry (Weinheim an Der Bergstrasse, Germany)
|December 6, 2012
PubMed
Summary

Researchers synthesized naphthalene diimides as DNA G-quadruplex alkylating agents. An oxirane derivative selectively alkylates adenine in G-quadruplex loops, forming a stable adduct.

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Single-molecule Manipulation of G-quadruplexes by Magnetic Tweezers
08:28

Single-molecule Manipulation of G-quadruplexes by Magnetic Tweezers

Published on: September 19, 2017

Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Molecular Biology

Background:

  • DNA G-quadruplexes are non-canonical DNA structures implicated in various biological processes.
  • Targeting G-quadruplexes offers potential therapeutic strategies for diseases like cancer.
  • Developing selective agents for G-quadruplexes remains a challenge.

Purpose of the Study:

  • To synthesize and investigate naphthalene diimide derivatives as selective DNA G-quadruplex alkylating agents.
  • To evaluate the potential of an oxirane-conjugated naphthalene diimide for G-quadruplex modification.

Main Methods:

  • Synthesis of naphthalene diimides conjugated to quinone methide and oxirane moieties.
  • Investigation of alkylating activity against DNA G-quadruplex structures.
  • Characterization of adduct formation and selectivity using biophysical and biochemical techniques.

Main Results:

  • Successful synthesis of novel naphthalene diimide conjugates.
  • The oxirane derivative demonstrated selective alkylation of G-quadruplex DNA.
  • Stable adduct formation was observed, specifically targeting adenine residues within G-quadruplex loops.

Conclusions:

  • Naphthalene diimide-oxirane conjugates are promising selective DNA G-quadruplex alkylating agents.
  • The oxirane derivative's ability to form stable, selective adducts highlights its therapeutic potential.
  • Further studies are warranted to explore the in vivo efficacy and applications of these compounds.