Martin J A
Department of Medicinal Chemistry, Roche Products Ltd., Welwyn Garden City, Hertfordshire, U.K.
Antiviral Res. 1992 Apr;17(4):265-78. doi: 10.1016/0166-3542(92)90022-w.
Inhibition of HIV proteinase is currently one of the most widely studied approaches for chemotherapeutic intervention in the treatment of AIDS. A range of inhibitors of this essential enzyme has been designed from detailed knowledge of its mechanism of action and cleavage sites. These inhibitors have been classified according to their derivation. All are transition-state analogues and contain a hydroxyethylene, hydroxyethylamine, phosphinate or symmetrical moiety. Many of these inhibitors have high selectivity for the viral enzyme and significant antiviral activity. Advances in the design of HIV proteinase inhibitors that have been reported in the past year are reviewed.
抑制HIV蛋白酶是目前治疗艾滋病化学治疗干预中研究最为广泛的方法之一。根据对这种关键酶作用机制和切割位点的详细了解，设计出了一系列该酶的抑制剂。这些抑制剂已根据其来源进行了分类。所有抑制剂都是过渡态类似物，含有羟乙烯、羟乙胺、次膦酸酯或对称部分。其中许多抑制剂对病毒酶具有高度选择性和显著的抗病毒活性。本文综述了过去一年中报道的HIV蛋白酶抑制剂设计方面的进展。
