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  • 标题:Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells
  • 本地全文:下载
  • 作者:J F Mayaux ; A Bousseau ; R Pauwels
  • 期刊名称:Proceedings of the National Academy of Sciences
  • 印刷版ISSN:0027-8424
  • 电子版ISSN:1091-6490
  • 出版年度:1994
  • 卷号:91
  • 期号:9
  • 页码:3564-3568
  • DOI:10.1073/pnas.91.9.3564
  • 语种:English
  • 出版社:The National Academy of Sciences of the United States of America
  • 摘要:A series of triterpene compounds characterized by a stringent structure-activity relationship were identified as potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1) replication. Currently studied botulinic derivatives have 50% inhibitory concentrations (IC50) against HIV-1 strain IIIB/LAI in the 10 nM range in several cellular infection assays but are inactive against HIV-2. These compounds did not significantly inhibit the in vitro activities of several purified HIV-1 enzymes. Rather, they appeared to block virus infection at a postbinding, envelope-dependent step involved in the fusion of the virus to the cell membrane.
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