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From Reverse to Forward Chemical Genomics: Development of Anti-HIV Agents

机译:从反向转发化学基因组学:抗HIV代理的发展

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摘要

To date, several anti-HIV agents have been developed based on reverse chemical genomics, in which target molecules are fixed. We found that CD4 mimic compounds have a great effect on the dynamic supramolecular mechanism of HIV entry, and that their combinational use with CXCR4 antagonists or with neutralizing antibodies shows a synergistic effect. On the other hand, based on forward chemical genomics, in which active compounds are searched according to the screening of random libraries, effective leads such as integrase inhibitors and matrix peptides have been found.
机译:迄今为止,已经基于逆向化学基因组学制定了几种抗HIV药物,其中固定了靶分子。我们发现CD4模拟化合物对HIV进入的动态超分子机制具有很大的效果,并且它们与CXCR4拮抗剂或中和抗体的组合使用表明了协同作用。另一方面,基于前向化学基因组学,根据随机文库的筛选搜查活性化合物,已经发现了诸如整容酶抑制剂和基质肽的有效铅。

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