XRAY CRYSTALLOGRAPHY OF INHIBITION OF SCHISTOSOMAL GLUTATHIONE S TRANSFERASE

血吸虫谷胱甘肽S转移酶抑制作用的X射线晶体学

• 批准号: 6658611
• 负责人: CHRISTOPHER M BRUNS
• 金额: $ 14.32万
• 依托单位: STANFORD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2002
• 资助国家: 美国
• 起止时间: 2002-03-01 至 2003-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6658611
• 关键词: bioimaging /biomedical imaging; biomaterials; biomedical resource; parasitism; proteins; radiography; structural biology

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.

血吸虫病是一种寄生虫病，可感染 200 多种 全世界有 100 万人死亡，每年死亡人数超过 200,000 人。 单人 治疗血吸虫病的主要药物是吡喹酮， 与血吸虫的谷胱甘肽 S-转移酶 (GST) 结合 粳稻。 因为血吸虫菌株具有抗药性 吡喹酮不断涌现，新型抗血吸虫药物的开发 需要化合物。 吡喹酮在一本小说中被证明具有结合作用 谷胱甘肽 S-转移酶的非底物结合位点。 我们的目标是 针对该位点开发改良的抗血吸虫药 药物。