Pyridoxal-5'-phosphate inhibits the polymerase activity of a recombinant RNAase H-deficient mutant of HIV-1 reverse transcriptase

AIDS Res Hum Retroviruses. 1992 May;8(5):597-604. doi: 10.1089/aid.1992.8.597.

Abstract

We have investigated the ability of pyridoxal-5'-phosphate to inhibit a recombinant deletion mutant of human immunodeficiency virus type 1(HIV-1) reverse transcriptase (RT) which is missing the last 23 amino acids of the C-terminus. This mutant reverse transcriptase is characterized by normal polymerase activity as compared with full-length enzyme; however, it has no RNase H activity. Inhibition studies with pyridoxal-5'-phosphate showed several differences as compared with inhibition of full-length enzyme: (1) Inhibition of mutant reverse transcriptase was independent of divalent cation, (2) Either substrate alone could protect mutant reverse transcriptase from inactivation by pyridoxal-5'-phosphate, and (3) stoichiometry of pyridoxal-5'-phosphate binding to mutant reverse transcriptase was 2 mol/mol under the same conditions in which 1 mol/mol bound to full-length enzyme. Furthermore, in the presence of either substrate alone, the stoichiometry of pyridoxal-5'-phosphate binding to the mutant was reduced to 1 mol/mol. These results indicate that the second binding site for pyridoxal-5'-phosphate seen in the mutant reverse transcriptase is at or near the primer-template binding site of the enzyme. They also suggest that the RNase H domain of HIV RT plays a functional role in substrate binding at the polymerase domain.

Publication types

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

MeSH terms

  • DNA-Directed DNA Polymerase / genetics
  • DNA-Directed DNA Polymerase / metabolism
  • HIV-1 / enzymology*
  • HIV-1 / genetics
  • Kinetics
  • Magnesium / metabolism
  • Mutation
  • Nucleic Acid Synthesis Inhibitors*
  • Pyridoxal Phosphate / pharmacology*
  • RNA-Directed DNA Polymerase / genetics
  • RNA-Directed DNA Polymerase / metabolism
  • Reverse Transcriptase Inhibitors*
  • Ribonuclease H / genetics
  • Ribonuclease H / metabolism*

Substances

  • Nucleic Acid Synthesis Inhibitors
  • Reverse Transcriptase Inhibitors
  • Pyridoxal Phosphate
  • RNA-Directed DNA Polymerase
  • DNA-Directed DNA Polymerase
  • Ribonuclease H
  • Magnesium