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逆转录酶在HIV感染的早期阶段起着重要作用,蛋白酶可催化病毒蛋白生成成熟的和具有感染力的病毒颗粒。因此,二者是抑制HIV复制的重要“靶酶”。HIV-1逆转录酶抑制剂和蛋白酶抑制剂由于药物毒性,口服生物利用度低以及病毒抗药性的出现而在临床上使用大受限制。为了寻找特异性强、疗效好的HIV抑制剂,作者筛选了一些巴拿马植物以观察它们对HIV逆转录酶和蛋白酶的抑制作用。
Reverse transcriptases play an important role in the early stages of HIV infection, and proteases catalyze the production of mature and infectious virus particles by viral proteins. Therefore, both are important “target enzymes” that inhibit HIV replication. HIV-1 reverse transcriptase inhibitors and protease inhibitors are greatly limited in clinical use because of their toxicity, low oral bioavailability, and the appearance of viral resistance. In an effort to find specific and effective HIV inhibitors, the authors screened several Panama plants to observe their inhibitory effect on HIV reverse transcriptase and protease.