Design, expression, and immunogenicity of a soluble HIV trimeric envelope fragment adopting a prefusion gp41 configuration

J Biol Chem. 2005 Jun 17;280(24):23138-46. doi: 10.1074/jbc.M414515200. Epub 2005 Apr 15.

Abstract

The human immunodeficiency virus-1 (HIV-1) envelope glycoprotein (Env) is comprised of non-covalently associated gp120/gp41 subunits that form trimeric spikes on the virion surface. Upon binding to host cells, Env undergoes a series of structural transitions, leading to gp41 rearrangement necessary for fusion of viral and host membranes. Until now, the prefusion state of gp41 ectodomain (e-gp41) has eluded molecular and structural analysis, and thus assessment of the potential of such an e-gp41 conformer to elicit neutralizing antibodies has not been possible. Considering the importance of gp120 amino (C1) and carboxyl (C5) segments in the association with e-gp41, we hypothesize that these regions are sufficient to maintain e-gp41 in a prefusion state. Based on the available gp120 atomic structure, we designed several truncated gp140 variants by including the C1 and C5 regions of gp120 in a gp41 ectodomain fragment. After iterative cycles of protein design, expression and characterization, we obtained a variant truncated at Lys(665) that stably folds as an elongated trimer under physiologic conditions. Several independent biochemical/biophysical analyses strongly suggest that this mini-Env adopts a prefusion e-gp41 configuration that is strikingly distinct from the postfusion trimer-of-hairpin structure. Interestingly, this prefusion mini-Env, lacking the fragment containing the 2F5/4E10 neutralizing monoclonal antibody binding sites, displays no detectable HIV-neutralizing epitopes when employed as an immunogen in rabbits. The result of this immunogenicity study has important implications for HIV-1 vaccine design efforts. Moreover, this engineered mini-Env protein should facilitate three-dimensional structural studies of the prefusion e-gp41 and serve to guide future attempts at pharmacologic and immunologic intervention of HIV-1.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antibodies, Monoclonal / chemistry
  • Baculoviridae / metabolism
  • Binding Sites
  • Cell Line
  • Cross-Linking Reagents / pharmacology
  • Dose-Response Relationship, Drug
  • Electrophoresis, Polyacrylamide Gel
  • Enzyme-Linked Immunosorbent Assay
  • Epitopes / chemistry
  • Gene Products, env / chemistry*
  • Gene Products, env / metabolism
  • Genes, Reporter
  • Genetic Vectors
  • Glycosylation
  • Green Fluorescent Proteins / metabolism
  • HIV Envelope Protein gp120 / chemistry
  • HIV Envelope Protein gp120 / metabolism
  • HIV Envelope Protein gp41 / chemistry*
  • HIV Envelope Protein gp41 / metabolism
  • HIV-1 / metabolism
  • Hydrogen-Ion Concentration
  • Immunoprecipitation
  • Insecta
  • Light
  • Luciferases / metabolism
  • Lysine / chemistry
  • Microscopy, Electron
  • Models, Biological
  • Models, Genetic
  • Models, Molecular
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Peptide Hydrolases / metabolism
  • Polysaccharides / chemistry
  • Protein Binding
  • Protein Conformation
  • Protein Engineering / methods
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Rabbits
  • Scattering, Radiation
  • Surface Plasmon Resonance
  • Time Factors
  • Trypsin / pharmacology
  • env Gene Products, Human Immunodeficiency Virus

Substances

  • Antibodies, Monoclonal
  • Cross-Linking Reagents
  • Epitopes
  • Gene Products, env
  • HIV Envelope Protein gp120
  • HIV Envelope Protein gp41
  • Polysaccharides
  • env Gene Products, Human Immunodeficiency Virus
  • gp140 envelope protein, Human immunodeficiency virus 1
  • Green Fluorescent Proteins
  • Luciferases
  • Peptide Hydrolases
  • Trypsin
  • Lysine