GS-5806 inhibits pre- to postfusion conformational changes of the respiratory syncytial virus fusion protein

  • Antimicrob Agents Chemother. 2015 Nov;59(11):7109-12. doi: 10.1128/AAC.00761-15.
Dharmaraj Samuel  1 ,  Weimei Xing  2 ,  Anita Niedziela-Majka  2 ,  Jinny S Wong  3 ,  Magdeleine Hung  2 ,  Katherine M Brendza  2 ,  Michel Perron  2 ,  Robert Jordan  2 ,  David Sperandio  2 ,  Xiaohong Liu  2 ,  Richard Mackman  2 ,  Roman Sakowicz  2
Affiliations
  • 1. Gilead Sciences, Inc., Foster City, California, USA [email protected].
  • 2. Gilead Sciences, Inc., Foster City, California, USA.
  • 3. Gladstone Institutes, University of California, San Francisco, California, USA.
PMID: 26324264 DOI: 10.1128/AAC.00761-15
Abstract

GS-5806 is a small-molecule inhibitor of human respiratory syncytial virus fusion protein-mediated viral entry. During viral entry, the fusion protein undergoes major conformational changes, resulting in fusion of the viral envelope with the host cell membrane. This process is reproduced in vitro using a purified, truncated respiratory syncytial virus (RSV) fusion protein. GS-5806 blocked these conformational changes, suggesting a possible mechanism for Antiviral activity.

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