XRAY CRYSTALLOGRAPHY OF INHIBITION OF SCHISTOSOMAL GLUTATHIONE S TRANSFERASE

$143,176P41FY2002RRNIH

Stanford University, Stanford CA

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Abstract

Schistosomiasis is a parasitic disease which infects over 200 million people worldwide, killing over 200,000 annually. The single major drug for treatment of schistosomiasis is praziquantel, which binds to the enzyme glutathione S-transferase (GST) from Schistosoma japonica. Because strains of Schistosoma that are resistant to praziquantel are emerging, the development of novel antischistosomal compounds is required. Praziquantel was shown to bind in a novel non-substrate binding site of glutathione S-transferase. We aim to target this site for the development of improved antischistosomal drugs.

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