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Antimalarial Effects of Human Immunodeficiency Virus Type 1 Protease Inhibitors Differ from Those of the Aspartic Protease Inhibitor Pepstatin

机译:人类免疫缺陷病毒1型蛋白酶抑制剂的抗疟作用与天冬氨酸蛋白酶抑制剂抑肽酶抑制素不同

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摘要

Human immunodeficiency virus type 1 protease inhibitors (HIVPIs) and pepstatin are aspartic protease inhibitors with antimalarial activity. In contrast to pepstatin, HIVPIs were not synergistic with a cysteine protease inhibitor or more active against parasites with the cysteine protease falcipain-2 knocked out than against wild-type parasites. As with pepstatin, HIVPIs were equally active against wild-type parasites and against parasites with the food vacuole plasmepsin aspartic proteases knocked out. The antimalarial mechanism of HIVPIs differs from that of pepstatin.
机译:人免疫缺陷病毒1型蛋白酶抑制剂(HIVPI)和胃蛋白酶抑制剂是具有抗疟疾活性的天冬氨酸蛋白酶抑制剂。与胃蛋白酶抑制素相反,HIVPI与半胱氨酸蛋白酶抑制剂没有协同作用,或者与被淘汰的半胱氨酸蛋白酶falcipain-2相比,对寄生虫的活性比对野生型寄生虫的活性更高。与胃蛋白酶抑制素一样,HIVPIs对野生型寄生虫和敲除食物液泡性溶酶的天冬氨酸蛋白酶的寄生虫同样具有活性。 HIVPIs的抗疟机制不同于胃酶抑素。

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