Brinkworth R I, Fairlie D P
Centre for Drug Design and Development, University of Queensland, Brisbane, Australia.
Biochim Biophys Acta. 1995 Nov 15;1253(1):5-8. doi: 10.1016/0167-4838(95)00183-u.
Quinones with one, two and three aromatic rings are a new class of micromolar non-peptidic inhibitors of HIV-1 proteinase, an enzyme essential for replication of Human Immunodeficiency Virus and an important drug target for AIDS. Substituted anthraquinones bearing hydroxyl substituents on one of their three rings were the most potent of these inhibitors. Comparisons with other small non-peptidic inhibitors that are now emerging, together with enzyme kinetic data indicating that alizarin is a competitive inhibitor, suggest that anthraquinones bind in the active-site groove of HIV-1 proteinase.
含有一个、两个和三个芳环的醌类是一类新型的微摩尔级非肽类HIV-1蛋白酶抑制剂，HIV-1蛋白酶是人类免疫缺陷病毒复制所必需的一种酶，也是治疗艾滋病的一个重要药物靶点。在其三个环之一上带有羟基取代基的取代蒽醌是这些抑制剂中活性最强的。与目前正在出现的其他小型非肽类抑制剂的比较，以及表明茜素是一种竞争性抑制剂的酶动力学数据表明，蒽醌类在HIV-1蛋白酶的活性位点凹槽中结合。
