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

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

  • Eur J Med Chem. 2015 Dec 1:106:34-43. doi: 10.1016/j.ejmech.2015.10.031.
Eva Rivero-Buceta 1,  Elisa G Doyagüez 1,  Ignacio Colomer 1,  Ernesto Quesada 1,  Leen Mathys 2,  Sam Noppen 2,  Sandra Liekens 2,  María-José Camarasa 1,  María-Jesús Pérez-Pérez 1,  Jan Balzarini 2,  Ana San-Félix 3
Affiliations

Affiliations

  • 1 Instituto de Química Médica (IQM-CSIC), Juan de la Cierva 3, 28006 Madrid, Spain.
  • 2 Rega Institute for Medical Research, KU Leuven, B-3000 Leuven, Belgium.
  • 3 Instituto de Química Médica (IQM-CSIC), Juan de la Cierva 3, 28006 Madrid, Spain. Electronic address: anarosa@iqm.csic.es.
PMID: 26513643 DOI: 10.1016/j.ejmech.2015.10.031
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.

Keywords

AIDS; Antiviral agents; HIV; Tryptophan.

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