能阻止1型人类免疫缺陷病毒进入细胞的三萜衍生物。
Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells.
作者信息
Mayaux J F, Bousseau A, Pauwels R, Huet T, Hénin Y, Dereu N, Evers M, Soler F, Poujade C, De Clercq E
机构信息
Rhône Poulenc Rorer S.A., Centre de Recherche de Vitry-Alfortville, Vitry Sur Seine, France.
出版信息
Proc Natl Acad Sci U S A. 1994 Apr 26;91(9):3564-8. doi: 10.1073/pnas.91.9.3564.
Abstract
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.
摘要
一系列具有严格构效关系的三萜化合物被鉴定为人类免疫缺陷病毒1型（HIV-1）复制的强效和选择性抑制剂。目前研究的肉毒杆菌衍生物在几种细胞感染试验中对HIV-1 IIIB/LAI株的50%抑制浓度（IC50）在10 nM范围内，但对HIV-2无活性。这些化合物并未显著抑制几种纯化的HIV-1酶的体外活性。相反，它们似乎在病毒与细胞膜融合所涉及的结合后、包膜依赖性步骤阻断病毒感染。
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