Translocation of a beta-peptide across cell membranes

J Am Chem Soc. 2002 Jan 23;124(3):368-9. doi: 10.1021/ja017283v.

Abstract

Short cationic peptides derived from DNA-binding proteins, of which HIV Tat is a prototype, can cross the membranes of living cells, and they can bring covalently attached moieties (proteins, drugs) along with them. We show that a beta-amino acid analogue of Tat 47-57 enters HeLa cells with comparable efficiency to Tat 47-57 itself (YGRKKRRQRRR). The beta-peptide is comprised of residues that bear the appropriate side chain at the beta-carbon. Both the alpha- and the beta-peptide were conjugated to fluorescein at the N terminus, and cell penetration was monitored by confocal fluorescence microscopy. Deletion of the three C-terminal arginine residues from the alpha-peptide abolished translocation activity, consistent with prior reports, and deletion of the three C-terminal beta3-homoarginine residues from the beta-peptide had a similarly adverse effect. Thus, alpha- and beta-peptide translocation processes show similar length/charge dependence. The beta-peptide appeared to be largely unfolded in water, which is consistent with the behavior of short Tat-derived alpha-peptides, but in methanol the beta-peptide adopted a helical conformation, in contrast to short Tat-derived alpha-peptides. Our results show that neither altering the oligomeric backbone (amide group spacing) nor increasing the intrinsic propensity to adopt a specific secondary structure affects translocation activity.

Publication types

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

MeSH terms

  • Cell Membrane / metabolism
  • Gene Products, tat / chemistry*
  • Gene Products, tat / metabolism*
  • HeLa Cells
  • Humans
  • Microscopy, Confocal
  • Oligopeptides / chemistry*
  • Oligopeptides / metabolism*
  • Peptide Fragments / chemistry*
  • Peptide Fragments / metabolism*
  • Protein Structure, Secondary
  • Structure-Activity Relationship

Substances

  • Gene Products, tat
  • Oligopeptides
  • Peptide Fragments