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Tight-binding inhibitors efficiently inactivate both reaction centers of monomeric Plasmodium falciparum glyoxalase 1

Glucose consumption and therefore methylglyoxal production of human erythrocytes increase significantly upon infection with malaria parasites. The glyoxalase systems of the host-parasite unit cope with this metabolic challenge by catalyzing the removal of harmful methylglyoxal. Thus, glyoxalase 1 fr...

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Main Authors: Urscher, Miriam (Author) , Alisch, Romy (Author) , Deponte, Marcel (Author)
Format: Article (Journal)
Language:English
Published: 19 May 2012
In: The FEBS journal
Year: 2012, Volume: 279, Issue: 14, Pages: 2568-2578
ISSN:1742-4658
DOI:10.1111/j.1742-4658.2012.08640.x
Online Access:Verlag, kostenfrei, Volltext: http://dx.doi.org/10.1111/j.1742-4658.2012.08640.x
Verlag, kostenfrei, Volltext: https://febs.onlinelibrary.wiley.com/doi/abs/10.1111/j.1742-4658.2012.08640.x
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Author Notes:Miriam Urscher, Swati S. More, Romy Alisch, Robert Vince and Marcel Deponte

MARC

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520 |a Glucose consumption and therefore methylglyoxal production of human erythrocytes increase significantly upon infection with malaria parasites. The glyoxalase systems of the host-parasite unit cope with this metabolic challenge by catalyzing the removal of harmful methylglyoxal. Thus, glyoxalase 1 from the malaria parasite Plasmodium falciparum (PfGlo1) could be a promising drug target. However, the enzyme has two different active sites and their simultaneous inactivation is considered challenging. Here, we describe the inactivation of PfGlo1 by two glyoxalase-specific tight-binding inhibitors with nanomolar Kiapp values and noncompetitive inhibition patterns. The inhibitors do not discriminate between the high-affinity and the high-activity conformations of PfGlo1, but seem to stabilize or trigger a conformational change in analogy with the substrate. In summary, we have characterized the most potent inhibitors of PfGlo1 known to date. 
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