A dimerization "switch" in the internalization mechanism of a cell-penetrating peptide

J Am Chem Soc. 2005 Jan 19;127(2):538-9. doi: 10.1021/ja0443171.

Abstract

The internalization mechanism of a cell-penetrating peptide has been explored through combinatorial selection of a phage-displayed peptide dimer library, chemical synthesis, and biophysical characterization. Both energy-dependent and energy-independent modes for peptide uptake by the target mammalian cells were observed, suggesting a role for higher-order structure in modulating the action of this novel cell-penetrating peptide.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • B-Lymphocytes / metabolism
  • Bacteriophages / metabolism
  • Cell Membrane / chemistry
  • Cell Membrane / metabolism
  • Cell Membrane Permeability
  • Dimerization
  • Enzyme-Linked Immunosorbent Assay
  • Microscopy, Fluorescence
  • Molecular Sequence Data
  • Oligopeptides / chemistry
  • Oligopeptides / metabolism*
  • Oligopeptides / pharmacokinetics
  • Peptide Library*
  • Protein Conformation
  • Proto-Oncogene Proteins c-jun / chemistry
  • Proto-Oncogene Proteins c-jun / metabolism
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / metabolism
  • Structure-Activity Relationship

Substances

  • Oligopeptides
  • Peptide Library
  • Proto-Oncogene Proteins c-jun
  • Recombinant Fusion Proteins