Approcci all'inibizione dell'aldolasi FBP di classe II
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Imported Edition - Ships in 18-21 Days
Free Shipping in India on orders above Rs. 500
L'aldolasi del fruttosio-1,6-bisfosfato (FBP) (E.C. 4.1.2.13) catalizza la condensazione aldolica reversibile del diidrossiacetonefosfato (DHAP) e del gliceraldeide-3-fosfato (G3P) nella glicolisi, nella gluconeogenesi e nel ciclo di Calvin. Le aldolasi FBP sono classificate in due gruppi in base ai diversi meccanismi catalitici. In particolare, l'aldolasi di classe II non � presente negli animali n� nelle piante, rendendo questo enzima un potenziale bersaglio farmacologico per organismi microbici patogeni come il Mycobacterium tuberculosis. � stato sintetizzato un substrato cromogenico come mimico dell'FBP. Il substrato cromogenico pu� essere utilizzato in un test cromogenico diretto per monitorare l'attivit� delle aldolasi FBP di Classe II e anche per valutare eventuali inibitori efficaci. Inoltre, il nostro gruppo di ricerca ha scoperto che un antidoto disponibile in commercio per l'avvelenamento da metalli pesanti, l'acido 2,3-dimercapto-1-propansolfonico (DMPS), � un buon inibitore competitivo dell'aldolasi FBP di Classe II. Al fine di migliorare l'affinit� di legame di questo inibitore nel sito attivo dell'enzima, sono state progettate razionalmente nuove molecole basate su questo composto utilizzando la modellazione molecolare.
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