Amprenavir is a selective HIV protease inhibitor with a Ki value of 0.6nM. The IC50 value of amprenavir against wild-type clinical HIV isolates in vitro is 14.6 ± 12.5ng/mL.[3] Treatment of Huh-7 cells with amprenavir (50μM) significantly inhibited invasion, blocked the conversion of latent MMP-2 to its 62/64-kD active form, but had no effect on cell proliferation compared to the DMSO-treated controls. Treatment with amprenavir via intragastric gavage (60 mg/kg/d, 5 days/week) for 3 weeks delayed tumor growth in nude mice inoculated with hepatoma Huh-7 cells.[4]
作用机制
Amprenavir prevents the virally encoded HIV protease from processing the cleavage of its natural substrates, gag and gag-pol polyproteins. It exerts the antiretroviral effect late in the HIV life cycle by interfering with virion maturation.[3]
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