Complexity in influenza virus targeted drug design: interaction with human sialidases.

Article Details

Citation

Copy to clipboard

Chavas LM, Kato R, Suzuki N, von Itzstein M, Mann MC, Thomson RJ, Dyason JC, McKimm-Breschkin J, Fusi P, Tringali C, Venerando B, Tettamanti G, Monti E, Wakatsuki S

Complexity in influenza virus targeted drug design: interaction with human sialidases.

J Med Chem. 2010 Apr 8;53(7):2998-3002. doi: 10.1021/jm100078r.

PubMed ID

20222714 [ View in PubMed

]

Abstract

With the global spread of the pandemic H1N1 and the ongoing pandemic potential of the H5N1 subtype, the influenza virus represents one of the most alarming viruses spreading worldwide. The influenza virus sialidase is an effective drug target, and a number of inhibitors are clinically effective against the virus (zanamivir, oseltamivir, peramivir). Here we report structural and biochemical studies of the human cytosolic sialidase Neu2 with influenza virus sialidase-targeting drugs and related compounds.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Oseltamivir	Sialidase-1	Protein	Humans	Unknown	Inhibitor	Details
Oseltamivir	Sialidase-2	Protein	Humans	Unknown	Inhibitor	Details
Zanamivir	Sialidase-2	Protein	Humans	Unknown	Inhibitor	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
2-deoxy-2,3-dehydro-N-acetylneuraminic acid	Sialidase-2	Ki (nM)	140000	N/A	N/A	Details
Zanamivir	Sialidase-2	Ki (nM)	17000	N/A	N/A	Details