Multiple enzymatic activities associated with recombinant NS3 protein of hepatitis C virus

J Virol. 1998 Aug;72(8):6758-69. doi: 10.1128/JVI.72.8.6758-6769.1998.

Abstract

The hepatitis C virus (HCV) nonstructural 3 protein (NS3) contains at least two domains associated with multiple enzymatic activities; a serine protease activity resides in the N-terminal one-third of the protein, whereas RNA helicase activity and RNA-stimulated nucleoside triphosphatase activity are associated with the C-terminal portion. To study the possible mutual influence of these enzymatic activities, a full-length NS3 polypeptide of 67 kDa was expressed as a nonfusion protein in Escherichia coli, purified to homogeneity, and shown to retain all three enzymatic activities. The protease activity of the full-length NS3 was strongly dependent on the activation by a synthetic peptide spanning the central hydrophobic core of the NS4A cofactor. Once complexed with the NS4A-derived peptide, the full-length NS3 protein and the isolated N-terminal protease domain cleaved synthetic peptide substrates with comparable efficiency. We show that, as in the case of the isolated protease domain, the protease activity of full-length NS3 undergoes inhibition by the N-terminal cleavage products of substrate peptides corresponding to the NS4A-NS4B and NS5A-NS5B. We have also characterized and quantified the NS3 ATPase, RNA helicase, and RNA-binding activities under optimized reaction conditions. Compared with the isolated N-terminal and C-terminal domains, recombinant full-length NS3 did not show significant differences in the three enzymatic activities analyzed in independent in vitro assays. We have further explored the possible interdependence of the NS3 N-terminal and C-terminal domains by analyzing the effect of polynucleotides on the modulation of all NS3 enzymatic functions. Our results demonstrated that the observed inhibition of the NS3 proteolytic activity by single-stranded RNA is mediated by direct interaction with the protease domain rather than with the helicase RNA-binding domain.

MeSH terms

  • Adenosine Triphosphatases / genetics
  • Adenosine Triphosphatases / isolation & purification
  • Adenosine Triphosphatases / metabolism*
  • Amino Acid Sequence
  • Gene Expression
  • Hepacivirus / enzymology*
  • Humans
  • Kinetics
  • Molecular Sequence Data
  • Protein Biosynthesis
  • RNA / metabolism
  • RNA Helicases
  • RNA Nucleotidyltransferases / genetics
  • RNA Nucleotidyltransferases / isolation & purification
  • RNA Nucleotidyltransferases / metabolism*
  • Recombinant Proteins / genetics
  • Recombinant Proteins / isolation & purification
  • Recombinant Proteins / metabolism
  • Serine Endopeptidases / genetics
  • Serine Endopeptidases / isolation & purification
  • Serine Endopeptidases / metabolism*
  • Substrate Specificity
  • Viral Nonstructural Proteins / genetics
  • Viral Nonstructural Proteins / isolation & purification
  • Viral Nonstructural Proteins / metabolism*

Substances

  • NS3 protein, hepatitis C virus
  • Recombinant Proteins
  • Viral Nonstructural Proteins
  • RNA
  • RNA Nucleotidyltransferases
  • Serine Endopeptidases
  • Adenosine Triphosphatases
  • RNA Helicases