2,3-didehydro-2,4-dideoxy-4-guanidino-N-acetyl-D-neuraminic acid (4-guanidino-Neu5Ac2en) is a slow-binding inhibitor of sialidase from both influenza A virus and influenza B virus.
The effect of 2,3-didehydro-2,4-dideoxy-4-guanidino-N-acetyl-D-neuraminic acid (4-guanidino-Neu5Ac2en) on the sialidases from influenza virus reassortant X31 (which contains the sialidase from A/Aichi/2/68) and influenza virus B/Beijing/1/87 has been investigated. We find that 4-guanidino-Neu5Ac2en is a slow-binding inhibitor of both influenza A and influenza B virus sialidase, and that association and dissociation rate constants are almost identical for both enzymes. Furthermore, values for these rate constants are independent of whether purified enzyme or detergent-treated virus is used in the assays.
Hart
G J
GJ
Department of Virology, Glaxo Research and Development Ltd., Glaxo Medicines Research Centre, Stevenage, Hertfordshire, U.K.
Bethell
R C
RC
D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000378:metabolism / Q000494:pharmacology*; D006146:Guanidines; D006801:Humans; D009980:Influenza A virus / Q000201:enzymology*; D009981:Influenza B virus / Q000201:enzymology*; D007700:Kinetics; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000302:isolation & purification / Q000378:metabolism; D011714:Pyrans; D012794:Sialic Acids / Q000378:metabolism / Q000494:pharmacology*; D013045:Species Specificity; D053243:Zanamivir
D004791:Enzyme Inhibitors; D006146:Guanidines; D011714:Pyrans; D012794:Sialic Acids; D009439:Neuraminidase; D053243:Zanamivir