HIV-1 ASPARTYL PROTEINASE RADIOPEPTIDASE ASSAY

为了帮助寻找对抗HIV-1病毒的有效药物， 引起艾滋病，一个方便的放射肽酶测定，建议用于 筛选这种负责传染性的酶的抑制剂。 HIV-1乙酰基蛋白酶是HIV-1的三种功能酶之一， 逆转录病毒，剪切翻译的gag-pol多肽（病毒基因产物） 感染细胞中的成熟病毒体。 抑制这种酶 阻止受感染病毒粒子的细胞增殖。 一个敏感 该酶的生化测定设计为使用放射性标记的 底物，当被乙酰基蛋白酶切割时， 在溶液中容易计数的标记的肽片段。 我们提出 建立和优化检测方法，并开始筛选 抑制剂的

As an aid in the search for effective drugs against the HIV-1 virus that causes AIDS, a convenient radiopeptidase assay is proposed to be used in the screening for inhibitors of this enzyme responsible for infectivity. The HIV-1 aspartyl proteinase, one of the 3 functional enzymes of the retrovirus, clips the translated gag-pol polypeptide (viral gene product) into the mature virions in the infected cell. Inhibition of this enzyme prevents the cellular multiplication of infected virions. A sensitive biochemical assay for this enzyme is designed using a radiolabeled substrate that when cleaved by the aspartyl proteinase generates a labeled peptide fragment that is easily counted in solution. We propose to establish and optimize the assay, as well as to start screening for inhibitors.