The active form of the influenza cap-snatching endonuclease inhibitor baloxavir marboxil is a tight binding inhibitor

B Todd, EP Tchesnokov, M Götte - Journal of Biological Chemistry, 2021 - ASBMB
Baloxavir marboxil (BXM) is an FDA-approved antiviral prodrug for the treatment of influenza
A and B infection and postexposure prophylaxis. The active form, baloxavir acid (BXA),
targets the cap-snatching endonuclease (PA) of the influenza virus polymerase complex.
The nuclease activity delivers the primer for transcription, and previous reports have shown
that BXA blocks the nuclease activity with high potency. However, biochemical studies on
the mechanism of action are lacking. Structural data have shown that BXA chelates the two …