Synthesis and biological evaluation of peptide mimics derived from first extracellular loop of CCR5 toward HIV-1.
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.
Ikeda
Kiyoshi
K
School of Pharmaceutical Sciences, University of Shizuoka, Yada, Shizuoka, Japan. ikeda@u-shizuoka-ken.ac.jp
Ishii
Yuko
Y
Konishi
Koji
K
Sato
Masayuki
M
Tanaka
Kiyoshi
K
D000595:Amino Acid Sequence; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D002855:Chromatography, Thin Layer; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008969:Molecular Sequence Data; D010455:Peptides / Q000494:pharmacology*; D019713:Receptors, CCR5 / Q000737:chemistry* / Q000187:drug effects; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013055:Spectrophotometry, Infrared
D019380:Anti-HIV Agents; D007202:Indicators and Reagents; D010455:Peptides; D019713:Receptors, CCR5