基于液相色谱-质谱联用技术对疟疾盒中一组抗疟药物进行初步筛选，以寻找恶性疟原虫硫氧还蛋白还原酶（PfTrxR）的抑制剂。
Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box.
作者信息
Tiwari Neil K, Reynolds Priscilla J, Calderón Angela I
机构信息
Department of Drug Discovery and Development, Auburn University, 4306 Walker Building, Auburn, AL 36849, USA.
出版信息
Molecules. 2016 Mar 28;21(4):424. doi: 10.3390/molecules21040424.
Plasmodium falciparum thioredoxin reductase (PfTrxR) has been identified as a potential drug target to combat growing antimalarial drug resistance. Medicines for Malaria Venture (MMV) has pre-screened and identified a set of 400 antimalarial compounds called the Malaria Box. From those, we have evaluated their mechanisms of action through inhibition of PfTrxR and found new active chemical scaffolds. Five compounds with significant PfTrxR inhibitory activity, with IC50 values ranging from 0.9-7.5 µM against the target enzyme, were found out of the Malaria Box.
恶性疟原虫硫氧还蛋白还原酶（PfTrxR）已被确定为应对日益增长的抗疟药物耐药性的潜在药物靶点。疟疾药物事业（MMV）已预先筛选并确定了一组名为“疟疾药盒”的400种抗疟化合物。从中，我们通过抑制PfTrxR评估了它们的作用机制，并发现了新的活性化学骨架。在“疟疾药盒”中发现了五种对PfTrxR具有显著抑制活性的化合物，其对目标酶的IC50值范围为0.9 - 7.5 μM。
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