Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors
Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors
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DOI：
10.1128/aac.40.7.1600
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发表时间：
1996-07-01
影响因子：
4.9
通讯作者：
Rasnick, D
中科院分区：
文献类型：
--
作者：
Rosenthal, PJ;Olson, JE;Rasnick, D
我们评估了乙烯基砜半胱氨酸蛋白酶抑制剂的抗疟作用，许多乙烯基砜强烈抑制恶性疟原虫半胱氨酸蛋白酶，是一种关键的血红蛋白酶。在培养寄生虫的研究中，纳摩尔浓度的三种乙烯基砜抑制寄生虫血红蛋白降解、代谢活性和发育，其抗疟作用与抑制镰刀菌蛋白酶相关。我们的结果表明，乙烯基砜或相关的半胱氨酸蛋白酶抑制剂可能有希望作为抗疟剂。
We evaluated the antimalarial effects of vinyl sulfone cysteine proteinase inhibitors, A number of vinyl sulfones strongly inhibited falcipain, a Plasmodium falciparum cysteine proteinase that is a critical hemoglobinase. In studies of cultured parasites, nanomolar concentrations of three vinyl sulfones inhibited parasite hemoglobin degradation, metabolic activity, and development, The antimalarial effects correlated with the inhibition of falcipain, Our results suggest that vinyl sulfones or related cysteine proteinase inhibitors may have promise as antimalarial agents.