β-羰基取代的谷胱甘肽缀合物作为旋盘尾丝虫谷胱甘肽S-转移酶2（O. volvulus GST2）的抑制剂
Beta-carbonyl substituted glutathione conjugates as inhibitors Of O. volvulus GST2.
作者信息
Brophy P M, Campbell A M, van Eldik A J, Teesdale-Spittle P H, Liebau E, Wang M F
机构信息
Institute of Biological Sciences, University of Wales, Ceredigion, UK.
出版信息
Bioorg Med Chem Lett. 2000 May 1;10(9):979-81. doi: 10.1016/s0960-894x(00)00142-6.
A series of beta-carbonyl substituted glutathione conjugates were prepared and evaluated as inhibitors of OvGST2. Their specificity for the parasite derived protein was assessed through comparison with their inhibition of human piGST. Inhibition of OvGST2 has been demonstrated at low micromolar concentrations for these conjugates and selectivity for OvGST2 over human pi-GST of greater than 10-fold has been achieved.
制备了一系列β-羰基取代的谷胱甘肽缀合物，并将其作为OvGST2的抑制剂进行评估。通过与它们对人piGST的抑制作用进行比较，评估了它们对寄生虫衍生蛋白的特异性。已证明这些缀合物在低微摩尔浓度下对OvGST2具有抑制作用，并且对OvGST2的选择性比对人pi-GST高10倍以上。
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