Three assays in one well: antimalarial compound library screening

Sheena McGowan Department of Biochemistry and Molecular Biology, Monash University 03/2013

The tropical disease malaria is caused by infection with Plasmodium parasites which use the host's metallopeptidases to degrade hemoglobin. The peptidases M1, M17 and M18 are associated with malaria and thus display a potential target of anti-malarial drugs.

Activity of the peptidases can be determined using synthetic substrates that release a dye upon cleavage by the active enzyme. The combination of a fluorophore-coupled substrate for M1 and M17 with a chromophore-coupled substrate for M18 measures the inhibitory potential of a compound on any of the three peptidases. Performing the assays on a BMG LABTECH multi-mode plate reader identified 25 compounds out of a 400 compound library to inhibit the peptidases M1 or M17.

Calculations were simplified by using the MARS Data Analysis Software with custom-tailored templates.

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