CD4 模拟物针对 HIV 进入机制。
CD4 mimics targeting the mechanism of HIV entry.
机构信息
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):354-8. doi: 10.1016/j.bmcl.2009.10.098. Epub 2009 Nov 4.
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.
进行了一系列 CD4 模拟小分子的构效关系研究，这些小分子可以阻断 HIV-1 gp120 与 CD4 之间的相互作用。这些 CD4 模拟物诱导 gp120 发生构象变化，暴露出其共受体结合位点。这与共受体 CXCR4 拮抗剂联合使用会产生高度协同作用，并揭示了 HIV-1 进入的动态超分子机制的显著影响。
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