Synthesis and biological evaluation of peptide mimics derived from first extracellular loop of CCR5 toward HIV-1

Chem Pharm Bull (Tokyo). 2004 Dec;52(12):1479-82. doi: 10.1248/cpb.52.1479.

Abstract

Peptide mimics derived from the first extracellular loop of CCR5 bearing non-peptide spacers in place of Ala-Ala-Ala sequence in the peptide moiety were synthesized, and the effects of these compounds on the inhibition against HIV-1 were examined. Compound 2b having m-aminophenoxyacetic acid derivative as a non-peptide spacer significantly inhibited HIV-1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / pharmacology*
  • Cell Line
  • Chromatography, Thin Layer
  • HIV-1 / drug effects*
  • Humans
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Molecular Sequence Data
  • Peptides / pharmacology*
  • Receptors, CCR5 / chemistry*
  • Receptors, CCR5 / drug effects
  • Spectrometry, Mass, Fast Atom Bombardment
  • Spectrophotometry, Infrared

Substances

  • Anti-HIV Agents
  • Indicators and Reagents
  • Peptides
  • Receptors, CCR5