Inhibition of human immunodeficiency virus type 1 tat-trans-activation-responsive region interaction by an antiviral quinolone derivative

Antimicrob Agents Chemother. 2004 May;48(5):1895-9. doi: 10.1128/AAC.48.5.1895-1899.2004.

Abstract

WM5, a 6-aminoquinolone derivative, binds with high affinity to the bulge of the trans-activation-responsive region (TAR), whereas it displays low binding affinity for the loop and stem regions of TAR and for random RNA and DNA sequences. Furthermore, WM5 disrupts the natural protein-nucleic acid complex with a 50% inhibitory concentration in the low micromolar range in both in vitro and in vivo assays.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Anti-HIV Agents / pharmacology*
  • Ciprofloxacin / analogs & derivatives
  • Ciprofloxacin / pharmacology*
  • DNA, Viral / drug effects
  • DNA, Viral / genetics
  • Gene Products, tat / antagonists & inhibitors*
  • Gene Products, tat / metabolism*
  • HIV Long Terminal Repeat / drug effects*
  • HIV Long Terminal Repeat / genetics
  • HIV-1 / drug effects
  • HIV-1 / metabolism*
  • Isoquinolines
  • Molecular Sequence Data
  • Mutation / genetics
  • Plasmids / genetics
  • Pyrroles
  • Quinolones / pharmacology*
  • RNA, Viral / drug effects
  • RNA, Viral / genetics
  • tat Gene Products, Human Immunodeficiency Virus

Substances

  • Anti-HIV Agents
  • DNA, Viral
  • Gene Products, tat
  • Isoquinolines
  • Pyrroles
  • Quinolones
  • RNA, Viral
  • WM5 compound
  • tat Gene Products, Human Immunodeficiency Virus
  • Ciprofloxacin