Antiviral activity and structural characteristics of the nonglycosylated central subdomain of human respiratory syncytial virus attachment (G) glycoprotein

J Biol Chem. 2001 Oct 19;276(42):38988-94. doi: 10.1074/jbc.M106288200. Epub 2001 Aug 3.

Abstract

Segments of the cystine noose-containing nonglycosylated central subdomain, residues 149-197, of the attachment (G) glycoprotein of human respiratory syncytial virus (HRSV) have been assessed for impact on the cytopathic effect (CPE) of respiratory syncytial virus (RSV). Nalpha-acetyl residues 149-197-amide (G149-197), G149-189, and G149-177 of the A2 strain of HRSV protected 50% of human epithelial HEp-2 cells from the CPE of the A2 strain at concentrations (IC(50)) between 5 and 80 microm. Cystine noose-containing peptides G171-197 and G173-197 did not inhibit the CPE even at concentrations above 150 microm. Systematic C- and N-terminal truncations from G149-189 and G149-177 and alanine substitutions within G154-177 demonstrated that residues 166-170 (EVFNF), within a sequence that is conserved in HRSV strains, were critical for inhibition. Concordantly, G154-177 of bovine RSV and of an antibody escape mutant of HRSV with residues 166-170 of QTLPY and EVSNP, respectively, were not inhibitory. Surprisingly, a variant of G154-177 with an E166A substitution had an IC(50) of 750 nm. NMR analysis demonstrated that G149-177 adopted a well-defined conformation in solution, clustered around F168 and F170. G154-170, particularly EVFNF, may be important in binding of RSV to host cells. These findings constitute a promising platform for the development of antiviral agents for RSV.

MeSH terms

  • Alanine / chemistry
  • Amino Acid Sequence
  • Animals
  • Antiviral Agents / pharmacology*
  • Cattle
  • Glycosylation
  • Humans
  • Inhibitory Concentration 50
  • Magnetic Resonance Spectroscopy
  • Membrane Glycoproteins / chemistry*
  • Models, Molecular
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Protein Binding
  • Protein Conformation
  • Protein Structure, Tertiary
  • Respiratory Syncytial Virus, Human / chemistry*
  • Sequence Homology, Amino Acid
  • Sheep
  • Viral Envelope Proteins / chemistry*

Substances

  • Antiviral Agents
  • G protein, Bovine respiratory syncytial virus
  • Membrane Glycoproteins
  • Peptides
  • Viral Envelope Proteins
  • glycoprotein O, Human respiratory syncytial virus
  • Alanine