Ansätze zur Hemmung der Klasse-II-FBP-Aldolase
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Imported Edition - Ships in 18-21 Days
Free Shipping in India on orders above Rs. 500
Fructose-1,6-bisphosphat (FBP)-Aldolase (E.C. 4.1.2.13) katalysiert die reversible Aldolkondensation von Dihydroxyacetonphosphat (DHAP) und Glyceraldehyd-3-phosphat (G3P) in der Glykolyse, der Glukoneogenese und im Calvin-Zyklus. FBP-Aldolasen werden anhand unterschiedlicher katalytischer Mechanismen in zwei Gruppen eingeteilt. Bemerkenswert ist, dass Aldolase der Klasse II weder in Tieren noch in Pflanzen vorkommt, was dieses Enzym zu einem potenziellen Wirkstoffziel f�r pathogene Mikroorganismen wie Mycobacterium tuberculosis macht. Als FBP-Mimetikum wurde ein chromogenes Substrat synthetisiert. Das chromogene Substrat kann in einem direkten chromogenen Assay zur �berwachung der Aktivit�t von FBP-Aldolasen der Klasse II sowie zur Bewertung geeigneter Inhibitoren eingesetzt werden. Dar�ber hinaus hat unsere Forschungsgruppe festgestellt, dass ein im Handel erh�ltliches Gegenmittel gegen Schwermetallvergiftungen, 2,3-Dimercapto-1-propansulfons�ure (DMPS), ein guter kompetitiver Inhibitor der FBP-Aldolase der Klasse II ist. Um die Bindungsaffinit�t dieses Inhibitors am aktiven Zentrum des Enzyms zu verbessern, wurden auf der Grundlage dieser Verbindung mithilfe molekularer Modellierung neue Molek�le rational entworfen.
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