Enzyme Inhibition Assay
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Authors
Chalouati, Khalil
Issue Date
2025-04-03
Type
Language
Keywords
Alternative Title
Abstract
Description
Influenza infections and virus mutations represent a major global health threat that
requires ongoing development of new and effective antiviral strategies. The only FDA
approved antiviral medications for the treatment of influenza are neuraminidase (NA)
inhibitors. NA cleaves glycosidic bonds from the surface of host cells, releasing new
progeny virions from infected cells during the final stage of a viral infection. The most
widely utilized method for testing NA inhibitors in vitro uses a fluorescence-based assay
and the substrate 2’-(4-Methylumbelliferyl)-α-D-N-acetylneuraminic acid (MUNANA).
Measuring the amount of fluorescent product, 4-methylumbelliferone (4-MU), produced
can be used to determine the potency of an NA inhibitor. Much of the work in our research
lab centers on the generation of weak NA inhibitors that can be used to screen the highly
virulent H1N1 strain of influenza. As such, we are modifying published procedures to
measure binding (IC50) in the micromolar range. Whole virus assays are common,
however we are testing on purified NA enzyme that can produce equivalent and potential
lead-generating results using a safer and cheaper alternative host.