Protein design of a bacterially expressed HIV-1 gp41 fusion inhibitor

Biochemistry. 2007 Apr 10;46(14):4360-9. doi: 10.1021/bi7001289. Epub 2007 Mar 20.

Abstract

Peptides derived from the carboxyl-terminal heptad repeat of the gp41 envelope glycoprotein ectodomain (C-peptides) can inhibit HIV-1 membrane fusion by binding to the amino-terminal trimeric coiled coil of the same protein. The fusion inhibitory peptide T-20 contains an additional tryptophan-rich sequence motif whose binding site extends beyond the gp41 coiled-coil region yet provides the key determinant of inhibitory activity in T-20. Here we report the design of a recombinant peptide inhibitor (called C52L) that includes both the C-peptide and tryptophan-rich regions. By calorimetry, C52L binds to a peptide mimic of the amino-terminal coiled coil with a Kd of 80 nM, reflecting the large degree of helicity in C52L as measured by circular dichroism spectroscopy. The C52L peptide potently inhibits in vitro infection of human T cells by diverse primary HIV-1 isolates irrespective of coreceptor preference, with nanomolar IC50 values. Significantly, C52L is fully active against T-20-resistant variants in a single-cycle HIV-1 infectivity assay. Moreover, because it can be expressed in bacteria, the C52L peptide might be more economical to manufacture on a large scale than T-20-like peptides produced by chemical synthesis. Hence the C52L fusion inhibitor may find a practical application, for example as a vaginal or rectal microbicide to prevent HIV-1 infection in the developing world.

Publication types

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

MeSH terms

  • Amino Acid Motifs
  • Amino Acid Sequence
  • Amino Acid Substitution
  • Animals
  • Anti-HIV Agents / pharmacology*
  • CHO Cells
  • Cell Fusion
  • Cell Line
  • Cells, Cultured
  • Coculture Techniques
  • Cricetinae
  • Cricetulus
  • Disulfides / chemistry
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Escherichia coli / genetics
  • HIV Envelope Protein gp41 / chemistry*
  • HIV Fusion Inhibitors / chemistry*
  • HIV Fusion Inhibitors / isolation & purification
  • HIV Fusion Inhibitors / metabolism
  • HIV Fusion Inhibitors / pharmacology
  • HIV-1 / physiology
  • Humans
  • Inhibitory Concentration 50
  • Leucine / metabolism
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / metabolism
  • Leukocytes, Mononuclear / virology
  • Models, Molecular
  • Molecular Sequence Data
  • Protein Engineering / methods*
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / metabolism
  • Tryptophan / chemistry
  • Virus Replication / drug effects

Substances

  • Anti-HIV Agents
  • Disulfides
  • HIV Envelope Protein gp41
  • HIV Fusion Inhibitors
  • Recombinant Fusion Proteins
  • Tryptophan
  • Leucine