Fumagillin suppresses HIV-1 infection of macrophages through the inhibition of Vpr activity |
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Authors: | Watanabe Nobumoto Nishihara Yoshifumi Yamaguchi Tomoyuki Koito Atsushi Miyoshi Hiroyuki Kakeya Hideaki Osada Hiroyuki |
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Institution: | Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2-1, Hirosawa, Wako, 351-0198, Japan. nwatanab@riken.jp |
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Abstract: | 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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Keywords: | HIV-1 human immunodeficiency virus type 1 Vpr viral protein R MetAP2 methionine aminopeptidases 2 |
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