蛋白酶抑制剂(英语:Protease inhibitor, antiprotease)是带有环状结构的肽化合物,可竞争性或非竞争性抑制蛋白酶活性,此外,蛋白酶抑制剂还可以降低白介素-1β转换酶的表达,从而使病毒颗粒无法成熟、抑制病毒的复制。FDA已批准上市7种药物(SQVRTVIDVNFVAPV等)。

自然界本就存在许多蛋白酶抑制剂,它们与蛋白酶互相制约而处于动态平衡;许多天然蛋白酶抑制剂本身结构也是蛋白质。蛋白酶抑制剂通过与蛋白酶活性位点结合调控靶蛋白酶活性,从而影响蛋白质代谢[1]

抗逆转录病毒药物

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The number of people in the U.S. dying of HIV fell by 60% in the 2 years following the introduction of the first HIV protease inhibitors

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