Designed metallopeptides as tools in chemical biology

  1. Barka , Ghofrane
Dirixida por:
  1. Marco Eugenio Vázquez Sentís Director
  2. Miguel Vázquez López Co-director

Universidade de defensa: Universidade de Santiago de Compostela

Fecha de defensa: 15 de decembro de 2017

Tribunal:
  1. Ignacio Alfonso Rodríguez Presidente/a
  2. Elena Pazos Secretario/a
  3. Fernando José López García Vogal
Departamento:
  1. Departamento de Química Orgánica

Tipo: Tese

Teseo: 517015 DIALNET HANDLE: https://hdl.handle.net/10347/16429
Minerva. Repositorio Institucional de la Universidad de Santiago de Compostela: lock_openAcceso aberto Handle

Resumo

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.