Rivero-Buceta Eva, Doyagüez Elisa G, Colomer Ignacio, Quesada Ernesto, Mathys Leen, Noppen Sam, Liekens Sandra, Camarasa María-José, Pérez-Pérez María-Jesús, Balzarini Jan, San-Félix Ana
Instituto de Química Médica (IQM-CSIC), Juan de la Cierva 3, 28006 Madrid, Spain.
Rega Institute for Medical Research, KU Leuven, B-3000 Leuven, Belgium.
Eur J Med Chem. 2015 Dec 1;106:34-43. doi: 10.1016/j.ejmech.2015.10.031. Epub 2015 Oct 21.
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.
已高效合成了在外围含有9至18个色氨酸残基的树枝状聚合物,并对其抗HIV复制的能力进行了测试。这些化合物抑制HIV复制周期的早期步骤,推测是病毒进入其靶细胞。我们的数据表明,通过本文所述化合物与HIV包膜糖蛋白gp120和gp41的优先相互作用,可防止HIV与宿主细胞上存在的(共)受体之间的相互作用,从而实现对HIV的抑制。目前获得的结果表明,外围9个色氨酸残基足以实现高效的gp120/gp41结合和抗HIV活性。