Peptide HIV-1 integrase inhibitors from HIV-1 gene products

J Med Chem. 2010 Jul 22;53(14):5356-60. doi: 10.1021/jm1003528.

Abstract

Anti-HIV peptides with inhibitory activity against HIV-1 integrase (IN) have been found in overlapping peptide libraries derived from HIV-1 gene products. In a strand transfer assay using IN, inhibitory active peptides with certain sequential motifs related to Vpr- and Env-derived peptides were found. The addition of an octa-arginyl group to the inhibitory peptides caused a remarkable inhibition of the strand transfer and 3'-end-processing reactions catalyzed by IN and significant inhibition against HIV replication.

Publication types

  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Cell Line
  • Cell Line, Tumor
  • Genes, Viral
  • HIV Integrase / chemistry
  • HIV Integrase Inhibitors / chemistry*
  • HIV Integrase Inhibitors / pharmacology
  • HIV-1 / drug effects
  • HIV-1 / genetics*
  • HIV-1 / physiology
  • Human Immunodeficiency Virus Proteins / chemistry*
  • Humans
  • Models, Molecular
  • Peptide Library*
  • Peptides / chemistry*
  • Peptides / pharmacology
  • Virus Replication / drug effects
  • env Gene Products, Human Immunodeficiency Virus / chemistry*
  • vpr Gene Products, Human Immunodeficiency Virus / chemistry*

Substances

  • HIV Integrase Inhibitors
  • Human Immunodeficiency Virus Proteins
  • Peptide Library
  • Peptides
  • env Gene Products, Human Immunodeficiency Virus
  • vpr Gene Products, Human Immunodeficiency Virus
  • HIV Integrase
  • p31 integrase protein, Human immunodeficiency virus 1