Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21228, USA.
Viruses. 2009 Dec;1(3):657-77. doi: 10.3390/v1030657. Epub 2009 Nov 4.
Although polypurine tract (PPT)-primed initiation of plus-strand DNA synthesis in retroviruses and LTR-containing retrotransposons can be accurately duplicated, the molecular details underlying this concerted series of events remain largely unknown. Importantly, the PPT 3' terminus must be accommodated by ribonuclease H (RNase H) and DNA polymerase catalytic centers situated at either terminus of the cognate reverse transcriptase (RT), and in the case of the HIV-1 enzyme, ∼70Å apart. Communication between RT and the RNA/DNA hybrid therefore appears necessary to promote these events. The crystal structure of the HIV-1 RT/PPT complex, while informative, positions the RNase H active site several bases pairs from the PPT/U3 junction, and thus provides limited information on cleavage specificity. To fill the gap between biochemical and crystallographic approaches, we review a multidisciplinary approach combining chemical probing, mass spectrometry, NMR spectroscopy and single molecule spectroscopy. Our studies also indicate that nonnucleoside RT inhibitors affect enzyme orientation, suggesting initiation of plus-strand DNA synthesis as a potential therapeutic target.
虽然逆转录病毒和含有 LTR 的逆转座子中的多嘧啶 tract (PPT)-引发的正链 DNA 合成可以被精确复制,但这一系列协同事件的分子细节在很大程度上仍不清楚。重要的是,核糖核酸酶 H (RNase H) 和位于互补逆转录酶 (RT) 两端的 DNA 聚合酶催化中心必须容纳 PPT 的 3'末端,而在 HIV-1 酶的情况下,两者之间的距离约为 70Å。因此,RT 和 RNA/DNA 杂交体之间的通讯似乎对于促进这些事件是必要的。虽然 HIV-1 RT/PPT 复合物的晶体结构提供了信息,但 RNase H 活性位点与 PPT/U3 连接点的距离有几个碱基对,因此对切割特异性的信息有限。为了填补生化和晶体学方法之间的差距,我们综述了一种结合化学探测、质谱、NMR 光谱和单分子光谱的多学科方法。我们的研究还表明,非核苷类 RT 抑制剂会影响酶的取向,这表明起始正链 DNA 合成是一个潜在的治疗靶点。