TRITERPENE DERIVATIVES THAT BLOCK ENTRY OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 INTO CELLS
TRITERPENE DERIVATIVES THAT BLOCK ENTRY OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 INTO CELLS
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DOI：
10.1073/pnas.91.9.3564
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发表时间：
1994-04-26
影响因子：
11.1
通讯作者：
LEPECQ, JB
中科院分区：
文献类型：
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作者：
MAYAUX, JF;BOUSSEAU, A;LEPECQ, JB
一系列具有严格构效关系的三萜化合物被确定为人类免疫缺陷病毒1型（HIV-1）复制的有效和选择性抑制剂。目前研究的白桦衍生物在几种细胞感染试验中对HIV-1株IIIB/LAI在10 nM范围内具有50%的抑制浓度（IC50），但对HIV-2无活性。这些化合物没有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的结合后、包膜依赖步骤中阻止病毒感染。
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 betulinic 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.