Status: Bibliographieeintrag
Standort: ---
Exemplare:
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| Online-Ressource |
Verfasst von: | Urscher, Miriam [VerfasserIn]  |
| Alisch, Romy [VerfasserIn]  |
| Deponte, Marcel [VerfasserIn]  |
Titel: | Tight-binding inhibitors efficiently inactivate both reaction centers of monomeric Plasmodium falciparum glyoxalase 1 |
Verf.angabe: | Miriam Urscher, Swati S. More, Romy Alisch, Robert Vince and Marcel Deponte |
E-Jahr: | 2012 |
Jahr: | 19 May 2012 |
Umfang: | 11 S. |
Teil: | volume:279 |
| year:2012 |
| number:14 |
| pages:2568-2578 |
| extent:11 |
Fussnoten: | Gesehen am 15.10.2018 |
Titel Quelle: | Enthalten in: Vereinigung der Europäischen Biochemischen GesellschaftenThe FEBS journal |
Ort Quelle: | Oxford [u.a.] : Wiley-Blackwell, 2005 |
Jahr Quelle: | 2012 |
Band/Heft Quelle: | 279(2012), 14, Seite 2568-2578 |
ISSN Quelle: | 1742-4658 |
Abstract: | 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. |
DOI: | doi:10.1111/j.1742-4658.2012.08640.x |
URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Kostenfrei: Volltext ; Verlag: http://dx.doi.org/10.1111/j.1742-4658.2012.08640.x |
| Kostenfrei: Volltext: https://febs.onlinelibrary.wiley.com/doi/abs/10.1111/j.1742-4658.2012.08640.x |
| DOI: https://doi.org/10.1111/j.1742-4658.2012.08640.x |
Datenträger: | Online-Ressource |
Sprache: | eng |
Sach-SW: | allosteric enzyme |
| drug development |
| glyoxalase |
| malaria |
| tight-binding inhibitor |
K10plus-PPN: | 158190276X |
Verknüpfungen: | → Zeitschrift |
Tight-binding inhibitors efficiently inactivate both reaction centers of monomeric Plasmodium falciparum glyoxalase 1 / Urscher, Miriam [VerfasserIn]; 19 May 2012 (Online-Ressource)
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