产品描述:
The antiviral agent Lopinavir is a potent inhibitor of HIV-1 protease (Ki=1.3pM for wild-type enzyme) and has been shown to block the replication of clinical isolates of HIV (EC50s=5-52nM). Lopinavir is an antiretroviral of the protease inhibitor class. It is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir (lopinavir/ritonavir). Lopinavir/ritonavir inhibits the HIV protease enzyme by forming an inhibitor-enzyme complex thereby preventing cleavage of the gag-pol polyproteins. Immature, non- infectious viral particles are subsequently produced. Lopinavir also has an ability to inhibit ZMPSTE24 (zinc metallopeptidase STE24). HIV-PIs block prelamin A processing by directly affecting the enzymatic activity of ZMPSTE24 and in this way they may contribute to lipodystrophy in individuals undergoing HIV-PI treatment. It also has been shown to inhibit meningioma cell proliferation, induce apoptosis on lymphoma cells and inhibit insulin signaling. Shown in a SARS-CoV-2 protease structure model study to potentially bind and inhibit the coronavirus endopeptidase C30 (CEP_C30) of SARS-CoV-2. A initial randomized trial study was not successful.