Larder B A, Purifoy D J, Powell K L, Darby G
Nature. 1987;327(6124):716-7. doi: 10.1038/327716a0.
Human immunodeficiency virus (HIV) is the causative agent of AIDS (acquired immune deficiency syndrome) a disease which poses a serious challenge to modern medicine. If we are to conquer this disease we will need a protective vaccine or effective drugs able to block the life cycle of the virus. An early stage in the invasion of the host cell is the conversion of the RNA genome of the virus to a double-stranded DNA intermediate which subsequently becomes integrated into the host cell chromosome. The enzyme reverse transcriptase is crucial in this process and is thus an obvious chemotherapeutic target. In this study we have used site-directed mutagenesis of this enzyme expressed in Escherichia coli to reveal several important functional regions of the protein including putative components of the triphosphate binding site and pyrophosphate exchange sites.
人类免疫缺陷病毒（HIV）是获得性免疫缺陷综合征（AIDS，艾滋病）的病原体，该疾病对现代医学构成了严峻挑战。如果我们要攻克这种疾病，就需要一种保护性疫苗或能够阻断病毒生命周期的有效药物。病毒入侵宿主细胞的早期阶段是将病毒的RNA基因组转化为双链DNA中间体，随后该中间体整合到宿主细胞染色体中。逆转录酶在这一过程中至关重要，因此是一个明显的化疗靶点。在本研究中，我们对在大肠杆菌中表达的这种酶进行了定点诱变，以揭示该蛋白质的几个重要功能区域，包括三磷酸结合位点和焦磷酸交换位点的假定组成部分。
