Characterization of a folding intermediate from HIV-1 ribonuclease H

Protein Sci. 1998 Oct;7(10):2164-74. doi: 10.1002/pro.5560071014.

Abstract

The RNase H domain from HIV-1 (HIV RNase H) encodes an essential retroviral activity. Refolding of the isolated HIV RNase H domain shows a kinetic intermediate detectable by stopped-flow far UV circular dichroism and pulse-labeling H/D exchange. In this intermediate, strands 1, 4, and 5 as well as helices A and D appear to be structured. Compared to its homolog from Escherichia coli, the rate limiting step in refolding of HIV RNase H appears closer to the native state. We have modeled this kinetic intermediate using a C-terminal deletion fragment lacking helix E. Like the kinetic intermediate, this variant folds rapidly and shows a decrease in stability. We propose that inhibition of the docking of helix E to this folding intermediate may present a novel strategy for anti HIV-1 therapy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Circular Dichroism
  • Deuterium / metabolism
  • Drug Design
  • Enzyme Inhibitors / chemistry
  • Enzyme Stability / drug effects
  • Guanidine / pharmacology
  • HIV-1 / enzymology*
  • Hydrogen / metabolism
  • Kinetics
  • Models, Molecular
  • Mutation / genetics
  • Protein Denaturation
  • Protein Folding*
  • Protein Structure, Secondary
  • Ribonuclease H / chemistry*
  • Viral Proteins / chemistry

Substances

  • Enzyme Inhibitors
  • Viral Proteins
  • Hydrogen
  • Deuterium
  • Ribonuclease H
  • Guanidine