期刊
FEBS LETTERS
卷 580, 期 11, 页码 2598-2602出版社
WILEY
DOI: 10.1016/j.febslet.2006.04.007
关键词
HIV-1; Vpr; AIDS; small molecule; fumagillin; cell cycle
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. (c) 2006 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
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