GS-5806 inhibits pre- to postfusion conformational changes of the respiratory syncytial virus fusion protein.
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.
Gilead Sciences, Inc., Foster City, California, USA dharmaraj.samuel@pfizer.com.
Dharmaraj
D
Samuel
Gilead Sciences, Inc., Foster City, California, USA.
Weimei
W
Xing
Gilead Sciences, Inc., Foster City, California, USA.
Anita
A
Niedziela-Majka
Gladstone Institutes, University of California, San Francisco, California, USA.
Jinny S
JS
Wong
Gilead Sciences, Inc., Foster City, California, USA.
Magdeleine
M
Hung
Gilead Sciences, Inc., Foster City, California, USA.
Katherine M
KM
Brendza
Gilead Sciences, Inc., Foster City, California, USA.
Michel
M
Perron
Gilead Sciences, Inc., Foster City, California, USA.
Robert
R
Jordan
Gilead Sciences, Inc., Foster City, California, USA.
David
D
Sperandio
Gilead Sciences, Inc., Foster City, California, USA.
Xiaohong
X
Liu
Gilead Sciences, Inc., Foster City, California, USA.
Richard
R
Mackman
Gilead Sciences, Inc., Foster City, California, USA.
Roman
R
Sakowicz
D000998:Antiviral Agents / Q000494:pharmacology*; D007191:Indazoles; D011487:Protein Conformation; D011720:Pyrazoles / Q000494:pharmacology*; D018357:Respiratory Syncytial Virus Infections; D018113:Respiratory Syncytial Virus, Human / Q000187:drug effects* / Q000378:metabolism*; D013449:Sulfonamides / Q000494:pharmacology*; D014764:Viral Proteins / Q000737:chemistry* / Q000378:metabolism*
D000998:Antiviral Agents; D007191:Indazoles; D011720:Pyrazoles; D013449:Sulfonamides; D014764:Viral Proteins; C000591241:presatovir