|
ИСТИНА |
Войти в систему Регистрация |
ФНКЦ РР |
||
Design of sodium channel ligands with defined selectivity - a case study in scorpion alpha-toxinsстатья Исследовательская статья
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: 10 октября 2019 г.
- Авторы: Kuldyushev Nikita A., Berkut Antonina A., Peigneur Steve, Tytgat Jan, Grishin Eugene V., Vassilevski Alexander A.
- Журнал: FEBS Letters
- Том: 591
- Номер: 20
- Год издания: 2017
- Издательство: Elsevier BV
- Местоположение издательства: Netherlands
- Первая страница: 3414
- Последняя страница: 3420
- DOI: 10.1002/1873-3468.12839
- Аннотация: Scorpion α-toxins are polypeptides that inhibit voltage-gated sodium channel inactivation. They are divided into mammal, insect and α-like toxins based on their relative activity toward different phyla. Several factors are currently known to influence the selectivity, which are not just particular amino acid residues but also general physical, chemical, and topological properties of toxin structural modules. The objective of this study was to change the selectivity profile of a chosen broadly active α-like toxin, BeM9 from Mesobuthus eupeus, toward mammal-selective. Based on the available information on what determines scorpion α-toxin selectivity, we designed and produced msBeM9, a BeM9 derivative, which was verified to be exclusively active toward mammalian sodium channels and, most importantly, toward the Nav 1.2 isoform expressed in the brain.
- Добавил в систему: Беркут Антонина Анатольевна