目前,批准用于治疗 AIDS 的抗病毒药物主要有黏附抑制剂(attachment inhibitors,AIs)、逆转录酶抑制剂(reverse transcriptase inhibitors,RTIs)、蛋白酶抑制剂(protease inhibitors,PIs)、整合酶抑制剂(integrase inhibitors,INs)、融合抑制...
Chapter 14. HIV Protease InhibitorsThe protease of the human immunodeficiency virus (HIV) is essential for cleavage of the viral gag and polypeptide precursors into individual structural proteins and enzymes during the final stage of viral maturation. Inhibitors of HIV protease have continued to ...
California. Intriguingly, while many other protease inhibitors are metabolized by CYP3A4, ritonavir is a potent mechanism-based inhibitor of both CYP3A4 and P-glycoprotein (Pgp), which shuttles the drug outside the cell....
California. Intriguingly, while many other protease inhibitors are metabolized by CYP3A4, ritonavir is a potent mechanism-based inhibitor of both CYP3A4 and P-glycoprotein (Pgp), which shuttles the drug outside the cell. Therefore, it could be used to increase plasma levels of co-dosed proteas...
蛋白酶抑制剂(Protease inhibitor,PIs)是肽类的化合物,是开发的第二类抗逆转录病毒药物,广泛用于治疗HIV / AIDS和丙型肝炎(HCV)。蛋白酶抑制剂通过选择性结合病毒蛋白酶(例如HIV-1特异天冬酰蛋白酶),并阻止产生感染性病毒颗粒所必需的蛋白质前体的蛋白水解裂解,来阻止病毒复制。
Biological Activity Lopinavir is a highly potent and selective HIV-1 protease inhibitor (IC50= 6.5 nM, HIV cultured in peripheral blood mononuclear cells; Ki= 1.3 pM). Displays >105-fold selectivity for HIV-1 protease over mammalian proteases including renin and cathepsin D and E. Inhibits HIV...
1.唾液中的分泌型白细胞蛋白酶抑制因子（secretory leukocyte protease inhibitor，SLPI)是唾液屏障的主要...
1 protease inhibitor (PI), OR 1 non-nucleoside reverse transcriptase inhibitor (NNRTI, "non-nuc"), OR 1 integrase strand transfer inhibitor (INSTI) What are nucleoside and nucleotide analog reverse transcriptase inhibitors (NRTIs)? When HIV infects CD4 cells, it converts its RNA to DNA using...
HIV protease inhibitors are potent anti-angiogenic molecules and promote regression of Kaposi sarcoma. Nat Med. 2002;8:225–32. Article CAS PubMed Google Scholar Hernández S, Catalán-García M, Morén C, García-Otero L, López M, Guitart-Mampel M, et al. Placental Mitochondrial Toxicity...
The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as we