Evaluation of mismatch-binding ligands as inhibitors for Rev-RRE interaction.
Evaluation of mismatch-binding ligands as inhibitors for Rev-RRE interaction.
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DOI：
10.1016/j.bmc.2006.03.038
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发表时间：
2006-08
影响因子：
3.5
通讯作者：
K. Nakatani;Souta Horie;Yuki Goto;A. Kobori;S. Hagihara
中科院分区：
文献类型：
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作者：
K. Nakatani;Souta Horie;Yuki Goto;A. Kobori;S. Hagihara
针对HIV-1mRNA的Rev负责元件(RRE)的茎环IIB的药物是治疗HIV-1感染的潜在药物。茎环的特征是由连续的G-G和G-A错配组成的内环，它是病毒mRNA核输出的REV蛋白的单一结合位点。我们在这里报道，在一个模型体系中，与双链DNA中G-G和G-A错配结合的配体也与REV肽竞争地结合到内环，并导致预先形成的REV-RRE复合体的解离。
Drugs targeting the stem-loop IIB of Rev responsible element (RRE) of HIV-1 mRNA are potential therapeutic agents for HIV-1 infection. The stem loop is characterized by an internal loop consist of consecutive G-G and G-A mismatches, which is the single binding site for Rev protein for nuclear export of viral mRNA. We report here that ligands binding to G-G and G-A mismatches in duplex DNA also bind to the internal loop in competition with Rev peptide and lead to the dissociation of pre-formed Rev–RRE complex in a model system.