Watanabe N, Nishihara Y, Yamaguchi T, Koito A, Miyoshi H, Kakeya
H, Osada H.Fumagillin suppresses HIV-1 infection of
macrophages through the inhibition of Vpr activity.
FEBS Lett. 2006 May 15;580(11):2598-602
Antibiotics Laboratory, Discovery Research Institute, RIKEN,
2-1, Hirosawa, Wako, 351-0198, Japan.
nwatanab@riken.jp
HIV-1 viral protein R (Vpr) is one of the human
immunodeficiency virus type 1 encoded proteins that have
important roles in viral pathogenesis. However, no clinical drug
for AIDS therapy that targets Vpr has been developed. Here, we
have established a screening system to isolate Vpr inhibitors
using budding yeast cells. We purified a Vpr inhibitory compound
from fungal metabolites and identified it as fumagillin, a
chemical already known to be a potent inhibitor of angiogenesis.
Fumagillin not only reversed the growth inhibitory activity of
Vpr in yeast and human cells, but also inhibited Vpr-dependent
viral gene expression upon the infection of human macrophages.
PMID: 16631749 |
