van Dongen MJP, et al. A small-molecule fusion inhibitor of influenza virus is orally active in mice. Science. 2019 Mar 8;363(6431).
Recent characterization of broadly neutralizing antibodies (bnAbs) against influenza virus identified the conserved hemagglutinin (HA) stem as a target for development of universal vaccines and therapeutics. Although several stem bnAbs are being evaluated in clinical trials, antibodies are generally unsuited for oral delivery. Guided by structural knowledge of the interactions and mechanism of anti-stem bnAb CR6261, we selected and optimized small molecules that mimic the bnAb functionality. Our lead compound neutralizes influenza A group 1 viruses by inhibiting HA-mediated fusion in vitro, protects mice against lethal and sublethal influenza challenge after oral administration, and effectively neutralizes virus infection in reconstituted three-dimensional cell culture of fully differentiated human bronchial epithelial cells. Cocrystal structures with H1 and H5 HAs reveal that the lead compound recapitulates the bnAb hotspot interactions.
See Also:
Latest articles in those days:
- [preprint]Egyptian rousette bat humoral immunity to H9 influenza hemagglutinin 13 hours ago
- The surveillance programme for avian influenza (AI) in Norwegian wildlife 2025 23 hours ago
- The surveillance programme for avian influenza (AI) in poultry in Norway 2025 23 hours ago
- Emergence of Novel Reassortant H3N2 Avian Influenza Viruses in Southern China: Genetic Complexity and Pathogenicity in Chickens and Mice 24 hours ago
- Pathological evidence of neurotropism and oculotropism in wild black-headed gulls naturally infected with H5N1 high pathogenicity avian influenza 1 days ago
[Go Top] [Close Window]


