HIV-1 ASPARTYL PROTEINASE RADIOPEPTIDASE ASSAY

HIV-1 天冬氨酰蛋白酶放射性肽酶测定

• 批准号: 3489658
• 负责人: MARTHA KNIGHT
• 金额: $ 5万
• 依托单位: PEPTIDE TECHNOLOGIES CORPORATION
• 依托单位国家: 美国
• 财政年份: 1993
• 资助国家: 美国
• 起止时间: 1993-05-01 至 1994-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3489658
• 关键词: antiAIDS agent; chromatography; drug screening /evaluation; exopeptidase; human immunodeficiency virus 1; method development; peptide chemical synthesis; peptide structure; protease inhibitor; radioassay; radiotracer; virus protein

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.

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