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Updated: Feb 16, 2026
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Single-Molecule Fluorescence Visualization of DNA Polymerase Dynamics at G-Quadruplexes
Published on: April 4, 2025
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Selective G-quadruplex binding by oligoarginine-Ru(dppz) metallopeptides
David Bouzada1, Iria Salvadó, Ghofrane Barka
1Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain. miguel.vazquez.lopez@usc.es.
Chemical Communications (Cambridge, England)
|January 5, 2018
Summary
Ruthenium(II) metallopeptides with octaarginine tails show a strong preference for binding DNA G-quadruplexes. These metallopeptides are internalized by cells, leading to apoptosis and cell death.
Area of Science:
- Coordination Chemistry
- Bioconjugate Chemistry
- Molecular Recognition
Background:
- Ruthenium(ii) complexes are explored for their potential in biological applications.
- Metallopeptides offer a versatile platform for drug delivery and diagnostics.
- DNA G-quadruplex structures are increasingly recognized as important targets in cancer therapy.
Purpose of the Study:
- To synthesize and characterize novel Ru(ii) metallopeptides with dppz ligands.
- To investigate the DNA binding properties of these metallopeptides, particularly their selectivity for G-quadruplex structures.
- To evaluate the cellular uptake and cytotoxic effects of the synthesized metallopeptides.
Main Methods:
- Solid-phase peptide synthesis (SPPS) for metallopeptide construction.
- Fluorescence titration assays for DNA binding studies.
- Cellular internalization and apoptosis assays.
Main Results:
- Successful synthesis of Ru(ii)-dppz metallopeptides.
- Metallopeptides with octaarginine tails exhibited a significant binding preference for DNA G-quadruplexes compared to those without.
- The interplay between octaarginine functionalization and ancillary ligands influenced DNA recognition.
- Oligoarginine metallopeptides were efficiently internalized by cells.
- Cellular uptake resulted in cell death with observable signs of apoptosis.
Conclusions:
- Octaarginine functionalization enhances the DNA G-quadruplex selectivity of Ru(ii)-dppz metallopeptides.
- These metallopeptides demonstrate potential as cytotoxic agents due to efficient cellular uptake and induction of apoptosis.
- The findings highlight the importance of functionalization in designing targeted metallodrugs.
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