HIV proteaseinhibitors: effectson viralmaturationand physiologic function in macrophages

摘要: Human immunodeficiency virus (HIV), the retrovirus believed to be cause of acquired immuno- deficiency syndrome (AIDS), infects a variety CD4� cells, including lymphocytes and cells mono- cyte/macrophage lineage. Encoded in HIV genome are several precursor proteins that must undergo proteo- lytic cleavage yield functional proteins. The gag protein (p55) is cleaved by virally en- coded aspartate protease (HIV protease). Because ofp55 required for viral maturation infec- tivity, inhibition an attractive target therapy designed block progression in- fection. Inhibitors from chemical classes have been synthesized antiviral ac- tivity has demonstrated monocyte/macrophage A few pro- tease inhibitors progressed clinic some shown promise early trials. There are, however, important issues will affect development successful inhibitor, cell tissue distribution immunotoxicity. These discussed, with emphasis on complexities posed J. Leukoc. Biol. 56: 374-380; 1994.