Evaluation of mismatch-binding ligands as inhibitors for Rev-RRE interaction |
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Authors: | Nakatani Kazuhiko Horie Souta Goto Yuki Kobori Akio Hagihara Shinya |
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Institution: | Department of Synthetic Chemistry and Biological Chemistry, Faculty of Engineering, Kyoto University, Kyoto 615-8510, Japan. nakatani@sanken.osaka-u.ac.jp |
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Abstract: | 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. |
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