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Fumagillin suppresses HIV‐1 infection of macrophages through the inhibition of Vpr activity
Author(s) -
Watanabe Nobumoto,
Nishihara Yoshifumi,
Yamaguchi Tomoyuki,
Koito Atsushi,
Miyoshi Hiroyuki,
Kakeya Hideaki,
Osada Hiroyuki
Publication year - 2006
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2006.04.007
Subject(s) - fumagillin , biology , yeast , virology , angiogenesis , biochemistry , cancer research
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.

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