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Synthesis, characterization and in vitro activity of thrombin-binding DNA aptamers with triazole internucleotide linkagesстатья
Статья опубликована в высокорейтинговом журнале
Информация о цитировании статьи получена из
Web of Science,
Scopus
Статья опубликована в журнале из списка Web of Science и/или Scopus
Дата последнего поиска статьи во внешних источниках: 22 декабря 2015 г.
- Авторы: Varizhuk Anna M., Tsvetkov Vladimir B., Tatarinova Olga N., Kaluzhny Dmitry N., Florentiev Vladimir L., Timofeev Edward N., Shchyolkina Anna K., Borisova Olga F., Smirnov Igor P., Grokhovsky Sergei L., Aseychev Anton V., Pozmogova Galina E.
- Журнал: European Journal of Medicinal Chemistry
- Том: 67
- Год издания: 2013
- Издательство: Elsevier BV
- Местоположение издательства: Netherlands
- Первая страница: 90
- Последняя страница: 97
- DOI: 10.1016/j.ejmech.2013.06.034
- Аннотация: A series of DNA aptamers bearing triazole internucleotide linkages that bind to thrombin was synthesized. The novel aptamers are structurally analogous to the well-known thrombin-inhibiting G-quadruplexes TBA15 and TBA31. The secondary structure stability, binding affinity for thrombin and anticoagulant effects of the triazole-modified aptamers were measured. A modification in the central loop of the aptamer quadruplex resulted in increased nuclease resistance and an inhibition efficiency similar to that of TBA15. The likely aptamer-thrombin binding mode was determined by molecular dynamics simulations. Due to their relatively high activity and the increased resistance to nuclease digestion imparted by the triazole internucleotide linkages, the novel aptamers are a promising alternative to known DNA-based anticoagulant agents.
- Добавил в систему: Tsvetkov Vladimir Borisovich