Design of a potent D-peptide HIV-1 entry inhibitor with a strong barrier to resistance

J Virol. 2010 Nov;84(21):11235-44. doi: 10.1128/JVI.01339-10. Epub 2010 Aug 18.

Abstract

The HIV gp41 N-trimer pocket region is an ideal viral target because it is extracellular, highly conserved, and essential for viral entry. Here, we report on the design of a pocket-specific D-peptide, PIE12-trimer, that is extraordinarily elusive to resistance and characterize its inhibitory and structural properties. D-peptides (peptides composed of D-amino acids) are promising therapeutic agents due to their insensitivity to protease degradation. PIE12-trimer was designed using structure-guided mirror-image phage display and linker optimization and is the first D-peptide HIV entry inhibitor with the breadth and potency required for clinical use. PIE12-trimer has an ultrahigh affinity for the gp41 pocket, providing it with a reserve of binding energy (resistance capacitor) that yields a dramatically improved resistance profile compared to those of other fusion inhibitors. These results demonstrate that the gp41 pocket is an ideal drug target and establish PIE12-trimer as a leading anti-HIV antiviral candidate.

Publication types

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

MeSH terms

  • Binding Sites
  • Drug Design*
  • Drug Resistance, Viral*
  • HIV Envelope Protein gp41 / antagonists & inhibitors
  • HIV Fusion Inhibitors / chemistry*
  • Peptide Hydrolases / metabolism
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Peptides / therapeutic use

Substances

  • HIV Envelope Protein gp41
  • HIV Fusion Inhibitors
  • Peptides
  • Peptide Hydrolases