MedElevator Войти в исследования
← Поиск публикаций

DOI 10.1016/j.bbrc.2026.153643

Медицинская библиотека · Biochemical and biophysical research communications · 2026

Virtual screening targeting the conserved domain of the IAV M2 protein reveals the potential broad-spectrum anti-IAV activity of ajmaline.

Chen Min, Chen Wenhuan, Jiang Xinyi, Liang Shaomei, Qin Yingqiao, Tang Jiayi, Li Yifei, Wu Qifan, Liang Xue, Wei Pengcheng, Liu Kunpeng, Luo Sulan

СтатьяПеревод в очереди

Аннотация

Influenza A virus (IAV) evolves rapidly through antigenic variation, leading to drug resistance and pandemic potential. To circumvent mutational escape, we employed a drug repurposing strategy targeting the evolutionarily conserved transmembrane domain (TMD) of the IAV M2 protein. Here, we report the discovery of Ajmaline, an antiarrhythmic alkaloid, as a broad-spectrum anti-IAV agent identified via virtual screening. Molecular docking and 100-ns dynamics simulations revealed stable binding across multiple IAV subtypes (H1N1, H2N2, H5N1, H7N9). The Cellular Thermal Shift Assay (CETSA) confirmed direct binding to both wild-type and N31S mutant M2 proteins. Ajmaline exhibited potent antiviral activity through dual mechanisms: direct inhibition of viral replication and upregulation of interferon-related genes (IFNB1, ISG56) coupled with suppression of apoptosis (Bax downregulation). In vivo, Ajmaline (15 mg/kg) improved survival to 83%, reduced pulmonary viral load, and alleviated lung pathology in H1N1-infected mice. These findings identify Ajmaline as a repurposed broad-spectrum antiviral candidate capable of overcoming existing drug resistance, providing a proof-of-concept for conserved-domain-targeting strategies in antiviral drug development.

Для цитирования: Chen Min, Chen Wenhuan, Jiang Xinyi, Liang Shaomei, Qin Yingqiao, Tang Jiayi, Li Yifei, Wu Qifan, Liang Xue, Wei Pengcheng, Liu Kunpeng, Luo Sulan. Virtual screening targeting the conserved domain of the IAV M2 protein reveals the potential broad-spectrum anti-IAV activity of ajmaline.. Biochemical and biophysical research communications. 2026. DOI: 10.1016/j.bbrc.2026.153643.

Предметные рубрики MeSH

Подготовка и перевод публикации
Обработка статьи · этапы, ошибки и управление
Загрузка состояния…

История · было → стало

Состояние обновляется каждые 5 секунд, пока блок открыт. Процент показывается только там, где известен объём работы. Пауза останавливает продолжение этапа; текущий запрос к источнику может завершиться.

Тип публикации указан по данным источника. Уровень доказательности автоматически не присваивается.