CD4 mimics targeting the mechanism of HIV entry

CD4 mimics targeting the mechanism of HIV entry
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DOI:
10.1016/j.bmcl.2009.10.098
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发表时间:
2010-01-01
影响因子:
2.7
通讯作者:
Tamamura, Hirokazu
Tamamura, Hirokazu
中科院分区:
医学4区
文献类型:
--
作者:
Yamada, Yuko;Ochiai, Chihiro;Tamamura, Hirokazu

文献摘要

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对几种模拟CD 4的小分子进行了结构-活性关系研究,这些小分子阻断HIV-1 gp 120和CD 4之间的相互作用。这些CD 4模拟物诱导gp 120的构象变化,暴露其共受体结合位点。这在与共受体CXCR 4拮抗剂组合使用中诱导高度协同的相互作用,并揭示了对HIV-1进入的动态超分子机制的显著作用。(C)2009爱思唯尔有限公司版权所有。
A structure-activity relationship study was conducted of several CD4 mimicking small molecules which block the interaction between HIV-1 gp120 and CD4. These CD4 mimics induce a conformational change in gp120, exposing its co-receptor-binding site. This induces a highly synergistic interaction in the use in combination with a co-receptor CXCR4 antagonist and reveals a pronounced effect on the dynamic supramolecular mechanism of HIV-1 entry. (C) 2009 Elsevier Ltd. All rights reserved.