Cellular uptake of highly-functionalized ruthenium(II) tris-bipyridine protein-surface mimetics

Bioorg Med Chem Lett. 2012 Jan 15;22(2):985-8. doi: 10.1016/j.bmcl.2011.12.007. Epub 2011 Dec 8.

Abstract

This manuscript describes cell-uptake studies with HEK 293T cells on a series of ruthenium complexes shown previously to act as receptors for protein surface recognition and was motivated by a desire to establish if these receptors represent suitable templates for further elaboration as inhibitors of protein-protein interactions. The results illustrate that large (>3000Da) highly functionalized anionic ruthenium complexes are efficiently transfected via endocytosis to lysosomes with negligible toxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2,2'-Dipyridyl / analogs & derivatives*
  • 2,2'-Dipyridyl / chemical synthesis
  • 2,2'-Dipyridyl / chemistry
  • 2,2'-Dipyridyl / pharmacokinetics
  • Cell Survival / drug effects
  • Coordination Complexes
  • Dose-Response Relationship, Drug
  • Endocytosis / drug effects
  • HEK293 Cells
  • Humans
  • Lysosomes / drug effects
  • Molecular Mimicry / drug effects*
  • Molecular Structure
  • Protein Binding / drug effects
  • Structure-Activity Relationship
  • Surface Properties

Substances

  • Coordination Complexes
  • tris(2,2-bipyridine)-ruthenium(II)
  • 2,2'-Dipyridyl