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聚酰胺-蝎形环番利特罗品选择性地结合富含 AT 的 DNA,而与配位金属的性质无关。

Polyamide-scorpion cyclam lexitropsins selectively bind AT-rich DNA independently of the nature of the coordinated metal.

机构信息

School of Chemistry, University of Sydney, Sydney, New South Wales, Australia.

出版信息

PLoS One. 2011 May 9;6(5):e17446. doi: 10.1371/journal.pone.0017446.

Abstract

Cyclam was attached to 1-, 2- and 3-pyrrole lexitropsins for the first time through a synthetically facile copper-catalyzed "click" reaction. The corresponding copper and zinc complexes were synthesized and characterized. The ligand and its complexes bound AT-rich DNA selectively over GC-rich DNA, and the thermodynamic profile of the binding was evaluated by isothermal titration calorimetry. The metal, encapsulated in a scorpion azamacrocyclic complex, did not affect the binding, which was dominated by the organic tail.

摘要

环巴胺首次通过一种合成上简便的铜催化“点击”反应连接到 1-、2-和 3-吡咯利托品上。合成并表征了相应的铜和锌配合物。配体及其配合物选择性地与富含 AT 的 DNA 而非富含 GC 的 DNA 结合,通过等温滴定量热法评估了结合的热力学特性。金属被封装在蝎子氮杂大环配合物中,不会影响结合,这主要由有机尾巴决定。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e57b/3090394/6221b5073728/pone.0017446.g001.jpg

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