PMID: 8615021Apr 1, 1996Paper

Inhibition of HIV infection by pseudopeptides blocking viral envelope glycoprotein-mediated membrane fusion and cell death

Virology
C CallebautA G Hovanessian

Abstract

The RP dipeptide motif is highly conserved in the third hypervariable region (V3 loop) of the extracellular envelope glycoprotein of different types of HIV isolates. In view of this, we have designed and synthesized a construction referred to as "template assembled synthetic peptide" (TASP), in which a lysine-rich short polypeptide was used as a template to covalently anchor arrays of tripeptides, such as RPR, RPK, or KPR. The pentavalent presentation, 5(RPR)-, 5(RPK)-, or 5(KPR)-TASP, molecules manifested maximum inhibitory activity on HIV infection with a 50% inhibitory concentration value of 1-5 microM, respectively. Structure and inhibitory-activity relationship studies using analogs of 5(KPR)-TASP indicated that the positively charged side chains of the K and R residues in the tripeptide molecules are critical for the optimal inhibitory activity of the pentavalent construct. Interestingly, replacement of L-amino acid residues by D-amino acids or reduction of the peptide bond between the first two amino acids of the tripeptide generated peptide-TASP analogs active at sub-microM, concentrations. The anti-HIV action of the peptide-TASP constructs is specific, since they inhibit infection of several types of CD4-expressing cel...Continue Reading

Citations

Mar 19, 1999·AIDS Research and Human Retroviruses·N SeddikiA G Hovanessian
Nov 8, 2001·Proceedings of the National Academy of Sciences of the United States of America·B KrustL Edelman
Jul 17, 1999·The Journal of Peptide Research : Official Journal of the American Peptide Society·M MoulardJ M Sabatier
Nov 26, 2008·Experimental Cell Research·Marie-Estelle LosfeldDominique Legrand
Aug 8, 2006·Chembiochem : a European Journal of Chemical Biology·Yashveer SinghPascal Dumy
Mar 30, 2001·Virology·C CallebautA G Hovanessian
Jun 11, 1999·Journal of Peptide Science : an Official Publication of the European Peptide Society·P Veprek, J Jezek
Jul 31, 2002·The Journal of Biological Chemistry·Elias A SaidAra G Hovanessian
Mar 14, 1997·The Journal of Biological Chemistry·C CallebautA G Hovanessian
Dec 1, 1998·The Journal of Peptide Research : Official Journal of the American Peptide Society·R BarboucheJ M Sabatier

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