Retroinverso analogue of the antiviral octapeptide C8 inhibits feline immunodeficiency virus in serum.
We described the antiviral activity of an octapeptide corresponding to a Trp-rich domain of feline immunodeficiency virus (FIV) transmembrane glycoprotein. To overcome the limited enzymatic stability of short peptides, the retroinverso analogue was prepared and tested for inhibitory activity of FIV in the presence or absence of normal cat serum. Differently from the unmodified peptide, the retroinverso analogue maintains strong inhibitory activity in serum. NMR studies showed that it displays crucial conformational features believed to be important for antiviral activity.
Department of Pharmaceutical Sciences, University of Salerno, I-84084 Fisciano, Italy.
Anna Maria
AM
D'Ursi
Simone
S
Giannecchini
Armida
A
Di Fenza
Cinzia
C
Esposito
Maria Rosaria
MR
Armenante
Alfonso
A
Carotenuto
Mauro
M
Bendinelli
Paolo
P
Rovero
D000818:Animals; D000998:Antiviral Agents / Q000097:blood / Q000138:chemical synthesis* / Q000494:pharmacology; D002415:Cats; D004355:Drug Stability; D016089:Immunodeficiency Virus, Feline / Q000737:chemistry / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D008562:Membrane Glycoproteins / Q000737:chemistry*; D008958:Models, Molecular; D008968:Molecular Conformation; D009842:Oligopeptides / Q000097:blood / Q000138:chemical synthesis* / Q000494:pharmacology; D012191:Retroviridae Proteins / Q000737:chemistry*; D014364:Tryptophan / Q000737:chemistry; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; D008562:Membrane Glycoproteins; D009842:Oligopeptides; D012191:Retroviridae Proteins; C474566:acetyl-tryptophyl-glutamyl-aspartyl-tryptophyl-valyl-glycyl-tryptophyl-isoleucinamide; D014364:Tryptophan