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Selective G-quadruplex binding by oligoarginine-Ru(dppz) metallopeptides
18
Citations
36
References
2017
Year
Chemical BiologyMedicinal ChemistrySelective G-quadruplex BindingBiochemistryG Protein-coupled ReceptorNatural SciencesMetalloproteinMolecular BiologyDppz LigandFluorescence Titration StudiesNon-peptide LigandMolecular RecognitionOligoarginine MetallopeptidesDrug Discovery
A set of Ru(ii) metallopeptides containing the dppz ligand has been synthesized using SPPS methods. Fluorescence titration studies show that those metallopeptides featuring an octaarginine tail display a large binding preference for DNA G-quadruplex structures over those lacking it, and also that the interplay between the octoarginine functionalization and the ancillary ligand in the complex has an essential role in the recognition process. Furthermore, the oligoarginine metallopeptides are also efficiently internalized, causing cell death with signs of apoptosis.
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