Modulation of hepatitis C virus NS3 protease and helicase activities through the interaction with NS4A

Biochemistry. 1999 Apr 27;38(17):5620-32. doi: 10.1021/bi982892+.

Abstract

The hepatitis C virus nonstructural 3 protein (NS3) possesses a serine protease activity in the N-terminal one-third, whereas RNA-stimulated NTPase and helicase activities reside in the C-terminal portion. The serine protease activity is required for proteolytic processing at the NS3-NS4A, NS4A-NS4B, NS4B-NS5A, and NS5A-NS5B polyprotein cleavage sites. NS3 forms a complex with NS4A, a 54-residue polypeptide that was shown to act as an essential cofactor of the NS3 protease. We have expressed in Escherichia coli the NS3-NS4A precursor; cleavage at the junction between NS3 and NS4A occurs during expression in the bacteria cells, resulting in the formation of a soluble noncovalent complex with a sub-nanomolar dissociation constant. We have assessed the minimal ionic strength and detergent and glycerol concentrations required for maximal proteolytic activity and stability of the purified NS3-NS4A complex. Using a peptide substrate derived from the NS5A-NS5B junction, the catalytic efficiency (kcat/Km) of NS3-NS4A-associated protease under optimized conditions was 55 000 s-1 M-1, very similar to that measured with a recombinant complex purified from eukaryotic cells. Dissociation of the NS3-NS4A complex was found to be fully reversible. No helicase activity was exhibited by the purified NS3-NS4A complex, but NS3 was fully active as a helicase upon dissociation of NS4A. On the other hand, both basal and poly(U)-induced NTPase activity and ssRNA binding activity associated with the NS3-NS4A complex were very similar to those exhibited by NS3 alone. Therefore, NS4A appears to uncouple the ATPase/ssRNA binding and RNA unwinding activities associated with NS3.

MeSH terms

  • Adenosine Triphosphatases / metabolism
  • Amino Acid Sequence
  • Binding Sites
  • DNA Helicases / metabolism*
  • Enzyme Activation / genetics
  • Escherichia coli / genetics
  • Hepacivirus / enzymology*
  • Kinetics
  • Macromolecular Substances
  • Molecular Sequence Data
  • Protein Biosynthesis
  • RNA, Viral / metabolism
  • Recombinant Proteins / biosynthesis
  • Recombinant Proteins / isolation & purification
  • Recombinant Proteins / metabolism
  • Serine Endopeptidases / genetics
  • Serine Endopeptidases / metabolism*
  • Substrate Specificity
  • Viral Nonstructural Proteins / genetics
  • Viral Nonstructural Proteins / isolation & purification
  • Viral Nonstructural Proteins / metabolism*

Substances

  • Macromolecular Substances
  • NS3 protein, hepatitis C virus
  • NS4 protein, hepatitis C virus
  • RNA, Viral
  • Recombinant Proteins
  • Viral Nonstructural Proteins
  • Serine Endopeptidases
  • Adenosine Triphosphatases
  • DNA Helicases