Designed metallopeptides as tools in chemical biology

• Autores: Ghofrane Barka
• Directores de la Tesis: Marco Eugenio Vázquez Sentís (dir. tes.), Miguel Vázquez López (codir. tes.)
• Lectura: En la Universidade de Santiago de Compostela ( España ) en 2017
• Idioma: inglés
• Tribunal Calificador de la Tesis: Ignacio Alfonso Rodríguez (presid.), Elena Pazos (secret.), Fernando José López García (voc.)
• Programa de doctorado: Programa de Doctorado en Ciencia y Tecnología Química por la Universidad de Santiago de Compostela y la Universidad de Vigo
• Materias:
  • Química
    • Bioquímica
      • Aminoácidos
      • Quimioterapia
      • Péptidos
    • Química inorgánica
      • Compuestos de coordinación
• Enlaces
  • Tesis en acceso abierto en: MINERVA
• Resumen

  • A series of Ru(II) metallopeptides featuring the dipyrido[3,2-a:2',3'-c]phenazine ligand (dppz) have been synthesized through solid-phase peptide synthesis (SPPS) methods. Spectroscopic studies indicate that functionalization with an oligoarginine basic tail causes a drastic change in the binding mode and a great increase of the affinity of these metallopeptides for well-matched B-DNA oligonucleotides over mismacthed DNAs. In addition, the spectroscopic data suggest that both the oligoarginine functionalization and the nature of the ancillary ligands do not cause an increase of the selectivity of these metallopeptides for a particular type of mismatched DNA oligonucleotide. Finally, fluorescence microscopy studies indicate that the oligoarginine functionalization causes the efficient internalization of the metallopeptides into Vero cells, causing apoptotic cell death after a few hours.