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Tryptophan dendrimers that inhibit HIV replication, prevent virus entry and bind to the HIV envelope glycoproteins gp120 and gp41.

Authors :
Rivero-Buceta E
Doyagüez EG
Colomer I
Quesada E
Mathys L
Noppen S
Liekens S
Camarasa MJ
Pérez-Pérez MJ
Balzarini J
San-Félix A
Source :
European journal of medicinal chemistry [Eur J Med Chem] 2015 Dec 01; Vol. 106, pp. 34-43. Date of Electronic Publication: 2015 Oct 21.
Publication Year :
2015

Abstract

Dendrimers containing from 9 to 18 tryptophan residues at the peryphery have been efficiently synthesized and tested against HIV replication. These compounds inhibit an early step of the replicative cycle of HIV, presumably virus entry into its target cell. Our data suggest that HIV inhibition can be achieved by the preferred interaction of the compounds herein described with glycoproteins gp120 and gp41 of the HIV envelope preventing interaction between HIV and the (co)receptors present on the host cells. The results obtained so far indicate that 9 tryptophan residues on the periphery are sufficient for efficient gp120/gp41 binding and anti-HIV activity.<br /> (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)

Details

Language :
English
ISSN :
1768-3254
Volume :
106
Database :
MEDLINE
Journal :
European journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
26513643
Full Text :
https://doi.org/10.1016/j.ejmech.2015.10.031