Institut für Organische Chemie und Chemische Biologie, Johann Wolfgang Goethe-Universität Frankfurt, Max-von-Laue-Strasse 7, 60438, Frankfurt am Main, Germany.
Chembiochem. 2016 Mar 15;17(6):506-14. doi: 10.1002/cbic.201500566. Epub 2016 Feb 16.
Bis(guanidinium)alcohols have been designed to react with phosphodiester substrates in a fast transphosphorylation step, a quasi-intramolecular process taking place in contact ion pairs. Here the attachment of such compounds to Dervan-type hairpin polyamides is described. The resulting conjugate 1 binds to AT-rich DNA duplexes with affinity similar to that of the parent polyamide as shown by UV melting experiments and CD titrations. Conjugate 1 nicks plasmid DNA at concentrations ranging from micromolar to high nanomolar.
双胍醇设计用于在快速的磷酸酯基转移反应步骤中与磷酸二酯底物反应，这是一个准分子内过程，发生在接触离子对中。本文描述了此类化合物与 Dervan 型发夹型聚酰胺的连接。如 UV 熔融实验和 CD 滴定所示，所得共轭物 1 与富含 AT 的 DNA 双链体的亲和力与亲本聚酰胺相似。共轭物 1 在从微摩尔到高纳摩尔的浓度范围内切割质粒 DNA。
